Term
|
Definition
Lincosamide
MOA: Block protein synthesis by bacterial
ribosomes
RES: 1) rRNA methylation/adenylation
2) altered ribosomal proteins
10% of topical application is
absorbed
SE: Bloody diarrhea
Pseudomembranous colitis
Tx: Acne vulgaris |
|
|
Term
|
Definition
| Polypeptide Cell Wall Inhibitor MOA: Binds membrane lipid carrier molecule → ↓ cell wall comp. Administer: topical (often w/neomycin & polymyxin B) SE: allergic contact dermatitis TX: Gram (+) bacteria, Anaerobes (cocci) |
|
|
Term
|
Definition
MOA: Produces compounds
toxic to DNA RES: (Rare, unknown mechanisms)
Administer: oral or IV
Distribution: great, CNS
SE: Possible carcinogen
Contraind: pregnancy & lactation ↓ elimination of lithium & ergot
derivatives...(no alcohol!)
TX: Effective against Dermodex brevis;
Anti-inflammatory; Acne rosacea |
|
|
Term
|
Definition
| MOA: Effective against most gram (+) Intranasal preparation SE: PEG vehicle can irritate nasal mucosa TX: Impetigo (S. aureus & S. pyogenes) |
|
|
Term
|
Definition
Aminoglycoside
MOA: 1) Block protein synthesis by
bacterial ribosomes
2) Disrupt magnesium bridges in
LPS
RES: 1) Modifying enzymes (most com.)
2) Efflux pumping
3) Altered ribosome binding
Administer: IM or IV (Topical here)
Post-ABX Effect: persistent
suppression after drug removal
Conc.-Dependent Killing:
↑ concentrations → better killing
SE: Nephrotoxicity, Ototoxicity (Streptomycin) (Mostly systemic administration) |
|
|
Term
|
Definition
| Effective against most gram (-) Topical TX: P. aeruginosa E. coli, enterobacter Klebsiella |
|
|
Term
|
Definition
Interax: benzos → ↑sedation
statins → rhabdomyolysis
SE: Gynecomastia
Hepatitis
Ventricular dysfx
TX: Chronic gen. MC candidiasis
Dermatophytes |
|
|
Term
|
Definition
Effective against dermatophyte
infection
Cream, shampoo, lotion, vagial
tablets, suppositories
Seborrheic dermatitis
Candidiasis |
|
|
Term
|
Definition
MOA: Effective against growing cells
Inhibits fungal cell wall synthesis
MET: Fine microcystal suspension
SE: Diarrhea
Photosensitivity
Headaches
Contraind: porphyria, liver dysfx TX: Tinea infections |
|
|
Term
|
Definition
Allylamines Anti-Fungal
MOA: Inhibit ergosterol synthesis
TX: Dermatophytes |
|
|
Term
|
Definition
Ointment Anti-Viral
MOA:
Guanine nucleoside analog
Viral thymidine kinase produces analog →
binds viral DNA polymerase & inactivates
MET: Valacyclovir −(rapidly)→ acyclovir
SE: Nausea, vomiting, diarrhea
Headache, renal dysfx
Resistance: altered/deficient viral
thymidine kinase or
viral DNA polymerase
TX: HSV
VZV |
|
|
Term
|
Definition
| Decreases viral shedding (time) & ↓time to healing Cream Applied at first sign of infection MOA: Guanine nucleoside analog Inhibits viral DNA synthesis Famciclovir is a prodrug metabolized to active penciclovir SE: Nausea, diarrhea Headache Tumors, testicular toxicity TX: Acute herpes zoster, Recurrent oro-labial HSV |
|
|
Term
|
Definition
Antiectoparasite
Shampoo or lotion
~Absorbed via skin, ↑in fatty tissue,
excreted in urine in 5 days
SE: Hematotoxicity (?)
Neurotoxicity
Pediculosis capitis
Pediculosis pubis
Scabies |
|
|
Term
|
Definition
Antiectoparasite
SE: Skin staining
Unpleasant odor
Lack of systemic effects
(good for kids and preggos)
TX: Scabies |
|
|
Term
|
Definition
Skin Pigmentation
MOA: Inhibit tyrosinase → ↓melanin →
↓skin hyperpigmentation
Hydroquinone = temporary
Monobenzone = permanent
SE: Local irritation
Allergy |
|
|
Term
|
Definition
Skin Pig.
MOA: Produce repigmentation of
depigmented macules
Psoralens intercalate w/DNA
SE: Skin cancer,
Cataracts
TX: Vitiligo |
|
|
Term
|
Definition
Sunscreen
MOA: blocks UV-light
SE: Skin Cancer (?) |
|
|
Term
|
Definition
Sunblock
MOA: Absorbs UV light
SE: creates carcinogenic free radicals, must be coated with silica/alumina |
|
|
Term
|
Definition
Tretinoin (ATRA)
MOA: ↓epidermis cohesion
↑cell turnover
Admin: topical
Applied to dry skin only
SE: Erythema
Dryness
Sunlight sensitivity
May appear worse in the first month,
as quiescent comedones emerge &
rupture
TX: Acne vulgaris (comedones)
Light-damaged skin |
|
|
Term
|
Definition
Naphtoic acid analog
MOA: Similar to retinoic acid but less
irritation
TX: Mild to moderate acne |
|
|
Term
|
Definition
MOA: Synthetic retinoid-like drug
Decreases sebaceous gland function
Admin: oral
SE: Similar to hypervitaminosis A:
dryness, itching, IBS
IBS, muscle pain, teratogen
TX: Severe cystic acne |
|
|
Term
|
Definition
Psoriasis
Admin: oral
TX: Psoriasis |
|
|
Term
|
Definition
| Psoriasis Anti-inflammatory Antiproliferative Extreme caution in young women (terotagenic) TX: Psoriasis |
|
|
Term
|
Definition
Psoriasis
MOA: Synthetic vitamin D3
SE: Skin dryness
Itching
TX: Psoriasis |
|
|
Term
|
Definition
MOA: Recomb. humanized monoclonal antibody binds CD11a, immunosuppressant, halts WBC chemotaxis into tissues Admin: SC weekly
SE: bacterial sepsis, viral meningitis, invasive fungal disease, progressive multifocal leukoencephalopathy caused by reactivation of latent JC virus
TX: Psoriasis |
|
|
Term
|
Definition
Glucocorticoid
MOA: Bind glucocorticoid receptors →
↑gluconeogenesis
↑glycogenesis
↑hormone-sensitive lipase
↑blood glucose
↓cytokines
↑vasoCX
demarginalized PMNs
↓vitamin D → ↓Ca2+ absorption &
Ca2+ clearance & ↑bone resorption
Admin: Inhaled SE: ↑susceptibility to infx
Inhibits growth in kids
Myopathy
Osteoporosis
Cataracts
Adrenocortical atrophy
Iatrogenic Cushing's
TX: Asthma
DERMATOLOGY
Anti-inflammatory
Antimitotic
SE: Skin atrophy, rosacea
↑IO pressure
Cushing's syndrome, growth
++Keloids, cystic acne, alopecia areata
= triamcinolone injection |
|
|
Term
|
Definition
Glucocorticoid
MOA:
Bind glucocorticoid receptors →
↑gluconeogenesis
↑glycogenesis
↑hormone-sensitive lipase
↑blood glucose
↓cytokines
↑vasoCX
demarginalized PMNs
↓vitamin D → ↓Ca2+ absorption &
↑Ca2+ clearance & ↑bone resorption
Admin: Short acting
SE:
↑susceptibility to infx
Inhibits growth in kids
Myopathy
Osteoporosis
Cataracts
Adrenocortical atrophy
Iatrogenic Cushing's
TX: Addison's Disease
DERMATOLOGY
Anti-inflammatory
Antimitotic
SE: Skin atrophy, rosacea
↑IO pressure
Cushing's syndrome, growth
Keloids, cystic acne, alopecia areata
= triamcinolone injection |
|
|
Term
|
Definition
Anti-Inflammatory
Byproducts of petrol distillation
Antipruritic
SE: Irritant folliculitis
Allergic contact dermatitis
TX: Psoriasis
Chronic lichenified dermatitis |
|
|
Term
|
Definition
Keratolytic
Solubilize cell surface protein debris
SE: Anaphylactic shock
Irritation & inflammation
Salicylism |
|
|
Term
|
Definition
| Anti-pruritic MOA: Potent histamine receptor (H1 & H2) antagonist Admin: oral or topical Allergic contact dermatitis SE: SE's & contraindications similar to anticholinergics TX: Atopic dermatitis Lichen simplex chronicus |
|
|
Term
|
Definition
Trichogenic
MOA: Reverses progressive ↓ of terminal
scalp hairs
Admin: topical
SE: Discontinuation causes continued hair
loss in 4-6 months
TX: Androgenic alopecia |
|
|
Term
|
Definition
Trichogenic
MOA: Blocks 5α-reductase → inhibits
conversion of testosterone → DHT
Admin: oral
SE: ↓libido
Ejaculation disorders
Eretctile dysfunction
Pregnant women should not be
exposed (hypospadias)
TX: Androgenic Alopecia |
|
|
Term
|
Definition
| Immunomodulator MOA: Inhibits calcineurin phosphatase → ↓ cytokines Impairs T-cell response to antigen Tacrolimus is 100x more potent (than cyclosporine) TX: GVHD (bone marrow trxpnt) Aplastic anemia (ineligible) Autoimmune disease; atopic dermatitis |
|
|
Term
|
Definition
| Immunomodulator MOA: unknown, stim. monocytes to release IFN-a and macros to release IL-1, IL-6, IL-8 and TNF-a; activates immune cells through Toll-like receptor 7 (TLR7); induces adaptive immune response SE: inflammation, dermatitis, eschars, tiredness, flu-like symptoms, diarrhea, fungal infections TX: Skin cancers, genital warts |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| GI Drug (H2 Blocker) MOA: Competitive inhibitor of histamine (H2)- stimulated gastric HCl secretion MET: Inhibits P450 system Drug interax: ↑chlordiazepoxide, EtOH propranolol, theophylline, warfarin SE: Diarrhea, muscle pain Headache, dizziness Gynecomastia, impotence TX: Gastric/duodenal ulcers ZE syndrome GERD |
|
|
Term
|
Definition
| GI drug (Proton Pump Inhib) MOA: Active form irreversibly binds & inhibits proton pump in parietal cells Absorbed in alkaline SI pH Use >2 months not advisable SE: Diarrhea, nausea Dizziness, headache Heals duodenal ulcers more rapidly than H2 blockers TX: Gastric/duodenal ulcers ZE syndrome GERD |
|
|
Term
|
Definition
| GI Drug (Mucosal Protectant) MOA: Aluminum salt of sucrose sulfate → binds plasma proteins in crater → protective barrier Short acting Drug interax: blocks tetracycline & PO4 absorption SE: Constipation Nausea Additionally: inhibits pepsin & bile aciton Also: ↑ prostaglandin release TX: Duodenal ulcer |
|
|
Term
|
Definition
| GI Drug (Cytoprotectant) MOA: Prostaglandin E1 analog → ↓ H+ ↑mucus & ↑bicarbonate secretion SE: Nausea, diarrhea Abortion in preggos TX: Gastric/duodenal ulcers NSAID-induced damage |
|
|
Term
|
Definition
| GI Drug (Mucosal Protectant/Antacid) MOA: React w/proteins in acid medium → protective barrier in ulcer crater SE: Black stools, black tongue Don't use in renal disease May have ABX activity against H. pylori TX: Gastric/duodenal ulcers |
|
|
Term
|
Definition
| GI Drug (Prokinetic Agent) MOA: Increases Peristalsis (via 5HT-3 Ach release), anti-nausea anti-emetic; D2 antagonist in the chemoreceptor trigger zone in CNS, 5-HT3 antagonist/5-HT4 agnoist (high dose) SE: Tardive Dyskinsea, Agranulocytosis, Neuroleptic-malignant Syndrome; restlessness, drowsiness, lassitude TX: Antiemetic, prokinetic |
|
|
Term
|
Definition
| GI Drug (Surfactant & Stool Softener) MOA: anionic surfactants widely used as emulsifying, wetting, and dispersing agents SE: increases Mg2 & K TX: makes stools softer/easier to pass |
|
|
Term
|
Definition
| GI Drug (Osmotic Laxative) MOA: antacid, mg2 supplement, short-term laxative SE: nausea & cramping; High doses = enterolith TX: Constipation, heartburn, sore stomach, osmotic emesis |
|
|
Term
|
Definition
| GI Drug (laxative) MOA: 5-HT4 agonist in the enteric nervous system in GI tract; 5-HT2b antagonist; induces peristalsis reduces GI pain SE: Increased risk of MI & Stroke (?) TX: Irritable bowl syndrome, constipation, |
|
|
Term
|
Definition
| GI Drug (antidiarrheal) MOA: diphenoxylate & atropine; diphenoxylate is a derivative of meperidine, an opiate which slows down GI tract through actions of peripheral mu-opiod receptors; and atropine prevents OD (with anti-emetic qualities) Contraindicated: Diphenoxylate/atropine allergy; jaundice; diarrhea to do Membranous Collitis, antibiotic trx, or diarrhea due to enterotoxin prod. bacteria Dx Interactions: Sedatives, Barbs, Benzos, Antidepressants, MAO-I's TX: Diarrhea |
|
|
Term
|
Definition
| GI Drug (antidiarrheal) MOA: u-opoid receptor agonist; decreases myenteric plexus activity; does NOT cross BBB (no analgesia) SE: slight physical dependence; Contraindicated: Fever; Bloody diarrhea due to invasive bactera (0157:H7 EHEC e.coli/salmonella) TX: diarrhea |
|
|
Term
|
Definition
| GI Drug (Irritable Bowl Syndrome) MOA: 5-HT3 antagonist of myenteric plexus; slows movement through bowel increasing H2O uptake & decreasing moisture/volume of fecal matter SE: withdrawn 2000 due to ischemic colitis; constipation, impaction, toxic megacolon TX: Irritable bowel syndrome (in women ONLY) |
|
|
Term
|
Definition
| GI Drug (Inflammatory Bowel) MOA: Bacteria split azo bond → 5-ASA (& sulfapyridine) → ↓ inflammation 75% reaches colon 5-ASA = active metabolite SE: Nausea, vomiting Headache Can cause ↓ folate absorption TX: Ulcerative colitis (85%) Colonic Crohn's Dz |
|
|
Term
|
Definition
| GI Drug (Inflammatory Bowel) MOA: Cytotoxins Low dose used for prophylaxis SE: Toxicity may limit chronic use Used in nonresponsive cases TX: Ulcerative colitis Crohn's disease |
|
|
Term
|
Definition
| GI Drug (Inflammatory Bowel) MOA: Inhibits DHFR → ↓ thymidylate, ↓ purines, ↓ methionine, ↓ serine CURES: osteosarcoma & choriocarcinoma ALL, Burkitt's, Non-H, Blad SE: Bone marrow (immunosupp) GI Nephro & Hepatotoxicity Develops resistance via DHFR , transport, MPs Also treats RA, psoriasis, & CROHN'S DISEASE Luke to the rescue (TMP has similar action) |
|
|
Term
|
Definition
| GI Drug (Inflammatory Bowel) MOA: Monoclonal antibody against TNF-α → ↓ inflammatory action Single IV infusion → remission SE: Nausea Serum sickness Infections, autoimmunity, cancer TX: Crohn's disease |
|
|
Term
|
Definition
| GI Drug (antiemetic) MOA: 5-HT3 receptor antagonist; reduces vagal tone to vomiting center in medulla oblongata; blocks 5-HT3 rec in chemoreceptor trigger zone SE: constipation, dizziness, headache TX: nausea/vomiting in chemotherapy |
|
|
Term
|
Definition
| GI Drug (antiemetic) MOA: substance P antagonist; neurokinin 1 receptor antagonist SE: few (?) Very specific for NK1 receptors TX: chemotherapy induced nausea/vomiting |
|
|
Term
|
Definition
| GI Drug (antiemetic) MOA: Block H1 receptor → ↓ histamine act. Allergies Motion sickness; Has Sedation Antiparkinsonian effects Anti-cholinergic effects Anti-serotonergic effects alpha receptor blocking Local anesthetic effects SE: Strong sedation! Ototoxicity (newborns or ABX) TX: Allergies MOTION SICKNESS (anti-chol./anti-5HT) Sedation |
|
|
Term
|
Definition
| GI Drug (antiemetic) MOA: D2 antagonist; Hist. antag; 5-HT antag SE: QT prolongation, Torsades TX: postoperative nausea/vomiting; antipsychotic |
|
|
Term
|
Definition
|
|
Term
|
Definition
| GI Drug (pancreatic enzyme) MOA: amylase, lipase, proteases, administered with each meal |
|
|
Term
|
Definition
| Endocrine (Growth Hormone) MOA: ↑IGF-1, ↑ECM, ↑muscle, ↑soft tissue, ↑urinary retention of nitrogen, PO4, K+, anti-insulin MET: Administered daily in evening (mimics normal pattern) SX: Children: few Adults: per. edema, arthralgia, myalgia, carpal tunnel syndrome TX: Childhood deficiency Adult deficiency |
|
|
Term
|
Definition
Endocrine (GnRH)
MOA: Binds GHRH receptor → ↑cAMP →
↑GH synthesis & release
MET: 40-80% of GH deficienct children
respond normally to GHRH
Hexorelin: ↑cardiac performance
(dilated cardiomyopathy)
TX: Dx pituitary defect
Hypothalamic GH deficiency |
|
|
Term
|
Definition
Endocrine (IGF)
MOA: Mitogenic & anti-apoptotic
Skeletal, muscle, organ growth
MET: Should not be used after closure of
epiphyses or in neoplasia
SX: May induce hypoglycemia
SPIGFD: mutations in GH receptor,
post GHR defect, IGF-1 defects
TX: Severe primary IGF
deficiency |
|
|
Term
|
Definition
Endocrine (Somatostatin)
MOA: Binds SRIF receptor → ↓cAMP →
↓GH release (synthesis intact)
Also inhibits TSH secretion
MET: Synthetic SRIF is resistant to
enzymes (t1/2: 3min→2hr)
Selective for GH (vs. insulin)
SE: ↓GI motility & secretions, ↓bile
production, ↓gallbladder CX
PVR of hypothalamus = 14 AAs
δ cells of pancreas = 28 AAs
TX: Acromegaly
Carcinoid tumors
VIPomas |
|
|
Term
|
Definition
Endocrine
MOA: GH lysine replaced by glycine → GH
antagonist
MET: PEGylated to ↑t1/2,
↓immunogenicity…but ↓affinity
(8 AA substitutions fix that)
SE: ↑hepatic aminotransferase
(otherwise well-tolerated)
Does not reduce size of GH tumor or
lower GH levels
TX: Acromegaly |
|
|
Term
|
Definition
Endocrine (ergot D2 agonist)
MOA: Paradoxical inhibitory effect on
somatroph adenomas (↓GH)
MET: Cabergoline > bromocriptine
SE: Headache, N/V, dizziness, postural
hypotension, insomnia
Most useful in ↑GH & ↑prolactin TX: Somatroph adenomas |
|
|
Term
|
Definition
Endocrine (ACTH)
MOA: CRH (hypothalamus) → ACTH (ant.
pituitary) → cortisol & aldosterone &
sex hormones
TX: Dx adrenal insufficiency |
|
|
Term
|
Definition
Endocrine (TSH)
MOA: Binds TSH receptor → ↑cAMP →
↑iodide uptake & TH syn/secr'n
TX: Dx residual thyroid
carcinoma |
|
|
Term
|
Definition
Endocrine (TRH)
MOA: Binds TRH receptor → ↑Ca2+ →
↑TSH & ↑prolactin
Admin: IV over 15-30 seconds
(TSH → 2-5x basal in 30 min)
SE: Transient nausea, hypo/HTN,
flushing, palpitations
TX: Dx 2° hypothyroidism
Measure PRL reserves |
|
|
Term
|
Definition
Endocrine (hCG)
MOA: Used for LH activity (acts at same
receptor as LH, but longer t1/2)
TX: Male infertility
Cryptorchidism
Dx Leydig cell failure |
|
|
Term
|
Definition
Endocrine (hMG)
MOA: Used for LH & FSH activity MET: IM OTH: Derived from urine of
postmenopausal women
TX: Male infertility
Female infertility |
|
|
Term
|
Definition
Endocrine (FSH)
MOA: Used for FSH activity (merotropin
w/LH component removed)
Urofollitropin: IM/subQ
rFSH: subQ
SE: Multiple births, ovarian
hyperstimulation syndrome, fluid
accumulation in cavities
TX: Female infertility |
|
|
Term
|
Definition
Endocrine (FSH)
MOA: Used for FSH activity (merotropin
w/LH component removed)
Urofollitropin: IM/subQ
rFSH: subQ
SE: Multiple births, ovarian
hyperstimulation syndrome, fluid
accumulation in cavities
TX: Female infertility |
|
|
Term
|
Definition
Endocrine (GnRH)
MOA: Binds GnRH receptor → ↑Ca2+ →
PLC → ↑FSH & ↑LH
MET: Long-acting agents (leuprolide,
histrelin, nafarelin, goserelin) have D-
AA's at cleavage site
SE: Hypogonadism, ↓bone
mineralization, ↑lipids
Pulsatile: ↑LH & FSH release
Continuous: ↓LH & FSH release
TX: GnRH deficiency
Delayed/precoc. Puberty
Gn-depen. Disease |
|
|
Term
|
Definition
Endocrine (GnRH long-acting)
MOA: Binds GnRH receptor → ↑Ca2+ →
PLC → ↑FSH & ↑LH
MET: Long-acting agents (leuprolide,
histrelin, nafarelin, goserelin) have D-
AA's at cleavage site
SE: Hypogonadism, ↓bone
mineralization, ↑lipids
Pulsatile: ↑LH & FSH release
Continuous: ↓LH & FSH release
TX: GnRH deficiency
Delayed/precoc. Puberty
Gn-depen. Disease |
|
|
Term
|
Definition
Endocrine (GnRH antag)
MOA: Competitive antagonists binding
GnRH receptor → ↓LH > ↓FSH ADMIN: subQ
No transient rise in gonadotropin
secretion as with continuous GnRH
administration
TX: Inhibit premature LH surge
in ovary stim. |
|
|
Term
|
Definition
| Endocrine (ADH) MOA: Binds V1a receptors → GI/vasoCX Binds V1b receptors → ↑ACTH Binds V2 receptors → ↑aquaporins V1 >> V2ADMIN: Nasal spray, subQ SE: VasoCX ↑GI muscle, ↑uterine muscle Desmopressin challenge: urine Osm should ↑50% w/central DI SIADH: Rx w/loop/demeclocycline Central diabetes insipidus TX: Dx central/nephro DI Post-op ileus...eso varices |
|
|
Term
|
Definition
| Endocrine (ADH) MOA: Binds V1a receptors → GI/vasoCX Binds V1b receptors → ↑ACTH Binds V2 receptors → ↑aquaporins; V2 >> V1 ADMIN: Nasal spray, subQ SE: VasoCX ↑GI muscle, ↑uterine muscle Desmopressin challenge: urine Osm should ↑50% w/central DI SIADH: Rx w/loop/demeclocycline Central diabetes insipidus TX: Dx central/nephro DI Post-op ileus...eso varices |
|
|
Term
|
Definition
Endocrine (Uterine)
MOA: binds G-protein rec. initiates phosphoinositol cascade → stimulates frequency and force of uterine smooth muscle contractions during parturition & causes contraction of mammary myoepithelial cells & milk ejection; powerful conx. of uterine arteries & veins
SE: uterine rupture, trauma, death of infant
TX: Induction of Labor, Test of uteroplacental insufficiency; maintain postpartum bleeding; increasing milk ejection during lactation |
|
|
Term
|
Definition
Endocrine (ergot uterine stimulant)
MOA: control postpartum bleeding when oxytocin not effective
SE: contraindicated in hypertensive patient, induce peripheral vasoconstriction |
|
|
Term
|
Definition
Endocrine (PGF2α analogue)
EYE: ↓ intraocular
pressure
VASC: vasocx
(↑ IP3 & ↑ Ca2+)
LUNG: bronchocx
(↑ IP3 & ↑ Ca2+)
REPRO: ↑ Uterine CX
(↑ oxytocin)
TX: control postpartum bleeding; elective abortion |
|
|
Term
|
Definition
Endocrine (PGE2 analogue)
EYE: ↓ intraocular
pressure
BLOOD: ↓ plt aggregation
VASC: vasodil + vasocx
(↑ IP3 & ↑ Ca2+)
LUNG: bronchodilation
(↑ cAMP)
GI: ↓ acid, ↑ mucus,
↑ blood
REPROD: ↓ tone
(+ ↑ oxy CX)
Kidney: ↑ blood,
↑ diuresis, ↓ ADH
CNS: ↑ body temp
↓ NE
TX: midtrimester elective abortion |
|
|
Term
|
Definition
| Admin: transdermal patch Most potent natural steroid Extensive first pass metabolism TOX: Endometrial hyperplasia Endometrial cancer Breast tenderness Feminization in males Cholestasis (GB disease) Hepatic adenomas ↑plasma TAG Thromboembolic disease/MI Headache, migraine BC Interax: ABX, phenytoin, barbiturates OTH: Ethinyl estradiol = #1 estrogen Norethidrone = #1 progestin Low-dose mono-triphasic = #1 ~ Suppress ovulation by negative feedback on gonadotropin release ~ Progestins = thicken cervical mucus ~ Thin endometrium ↓ ovum transport ~ ↑hormone binding proteins ↑insulin secretion & resistance |
|
|
Term
|
Definition
| Endocrine Synthetic steroidal estrogens Admin: IM (x1/month) Insoluble in water SE: Endometrial hyperplasia Endometrial cancer Breast tenderness Feminization in males Cholestasis (GB disease) Hepatic adenomas ↑plasma TAG Thromboembolic disease/MI Headache, migraine BC Interax: ABX, phenytoin, barbiturates Ethinyl estradiol = #1 estrogen Norethidrone = #1 progestin Low-dose mono-triphasic = #1 ~ Suppress ovulation by negative feedback on gonadotropin release ~ Progestins = thicken cervical mucus ~ Thin endometrium ↓ ovum transport ~ ↑hormone binding proteins ↑insulin secretion & resistance TX: Oral contraceptive Hormone replacement (Primary hypogonadism) |
|
|
Term
|
Definition
| Endocrine (conjugated natural estrogen) Sulfate ester of estrone Conjugated & esterified natural steroids Admin: IM Endometrial hyperplasia Endometrial cancer Breast tenderness Feminization in males Cholestasis (GB disease) Hepatic adenomas ↑plasma TAG Thromboembolic disease/MI Headache, migraine BC Interax: ABX, phenytoin, barbiturates Ethinyl estradiol = #1 estrogen Norethidrone = #1 progestin Low-dose mono-triphasic = #1 ~ Suppress ovulation by negative feedback on gonadotropin release ~ Progestins = thicken cervical mucus ~ Thin endometrium ↓ ovum transport ~ ↑hormone binding proteins ↑insulin secretion & resistance TX: Hormone replacement (Primary hyogonadism) Prostate cancer |
|
|
Term
|
Definition
| Endocrine Synthetic steroidal estrogens Admin: PO ↓ first pass metabolism (ethinyl) Endometrial hyperplasia Endometrial cancer Breast tenderness Feminization in males Cholestasis (GB disease) Hepatic adenomas ↑plasma TAG Thromboembolic disease/MI Headache, migraine BC Interax: ABX, phenytoin, barbiturates Ethinyl estradiol = #1 estrogen Norethidrone = #1 progestin Low-dose mono-triphasic = #1 ~ Suppress ovulation by negative feedback on gonadotropin release ~ Progestins = thicken cervical mucus ~ Thin endometrium ↓ ovum transport ~ ↑hormone binding proteins ↑insulin secretion & resistance TX: Oral contraceptive Hormone replacement (Primary hypogonadism) |
|
|
Term
|
Definition
| Endocrine (estrogen receptor modulators) Partial estrogen agonist (competitive inhibitor of ER) Admin: oral x5 days SE: Ovarian enlargement, vasomotor flushing, OHSS OTHER: ↑amplitude (not frequency) of pulsatile LH & FSH secretion TX: Induce ovulation Dx gonadotropin secr'n |
|
|
Term
|
Definition
| Endocrine (estrogen receptor modulators) Pure estrogen receptor antagonist → ER downregulation Admin: IM (x1/month) As effective as anastrozole TX: ER+ metastatic breast cancer |
|
|
Term
|
Definition
| Endocrine (estrogen receptor modulator) Breast: estrogen antagonist Lipids, bones, uterus: agonist TX: ER+ breast cancer |
|
|
Term
|
Definition
| Endocrine (estrogen receptor modulator) anti-estrogen on breast and uterus; estrogen on lipids, bones; ↓total cholesterol ↓risk of breast cancer Osteoporosis (in post-menopausal) |
|
|
Term
|
Definition
| Endocrine (3rd Generation 19-nortestosterone derivative Progestin) MOA: diffuses into cell, binds to PR between cytoplasmic and nuclear domains, forms homo- and hetero-dimers, which bind to response elements similar to glucocorticoids. The only role of the progestin component of combination oral contraceptives is to protect endometrium from estrogen-induced hyperplasia & cancer SE: (Less androgen activity with 3rd gen.) ↑fat deposition & weight gain Acne Menstrual abnormalities Uterine cramps Hirsutism (androgenic preps) ↑risk of breast cancer TX: Oral contraceptive Suppress gonadotropins |
|
|
Term
|
Definition
Endocrine (21-carbon derivative Progestin)
MOA: MOA: diffuses into cell, binds to PR between cytoplasmic and nuclear domains, forms homo- and hetero-dimers, which bind to response elements similar to glucocorticoids. The only role of the progestin
component of combination oral
contraceptives is to protect
endometrium from estrogen-induced
hyperplasia & cancer
Admin: IM
>oral activity than progesterone
The only role of the progestin
component of combination oral
contraceptives is to protect
endometrium from estrogen-induced
hyperplasia & cancer
SE:
↑fat deposition & weight gain
Acne
Menstrual abnormalities
Uterine cramps
Hirsutism (androgenic preps)
↑risk of breast cancer
TX: Endometrial protection in estrogen therapy/Ovarian suppression for dysmenorrhea, endometriosis & vaginal bleeding disorders |
|
|
Term
|
Definition
Endocrine (19-Nortestosterone derivative)
MOA: diffuses into cell, binds to PR between cytoplasmic and nuclear domains, forms homo- and hetero-dimers, which bind to response elements similar to glucocorticoids. The only role of the progestin
component of combination oral
contraceptives is to protect
endometrium from estrogen-induced
hyperplasia & cancer
SE: ↑fat deposition & weight gain
Acne
Menstrual abnormalities
Uterine cramps
Hirsutism (androgenic preps)
↑risk of breast cancer
TX: Oral contraceptive
Suppress gonadotropins |
|
|
Term
|
Definition
Endocrine
MOA: diffuses into cell, binds to PR between cytoplasmic and nuclear domains, forms homo- and hetero-dimers, which bind to response elements similar to glucocorticoids. The only role of the progestin
component of combination oral
contraceptives is to protect
endometrium from estrogen-induced
hyperplasia & cancer
SE:
↑fat deposition & weight gain
Acne
Menstrual abnormalities
Uterine cramps
Hirsutism (androgenic preps)
↑risk of breast cancer
TX: Endometrial protection in estrogen therapy/Ovarian suppression for dysmenorrhea, endometriosis & vaginal bleeding disorders |
|
|
Term
|
Definition
Endocrine (PR & ER antagonist)
MOA: Competitive binding to progesterone
receptor & ↓prostaglandin
dehydrogenase
MET: Inh. prog receptor & ↑PG → uteroCX
Given w/misoprostol 2 days later
Also blocks glucocorticoid receptor
TX: Abortifacient
Cushing syndrome |
|
|
Term
|
Definition
Endocrine (Thyroid)
MOA: Identical to endogenous T4
Converted to T3
Intrx: steroids, tmxfn, opioid, 5-FU,
phenytoin, CPZ, salicylate, benzos
Contraind: adrenal insufficiency
SE: Nervousness, arrhythmia, HTN,
SOB, N/V, diarrhea, heat intolerance,
↓reproductive fx
OTHER: ↑TBG in children & preggos →
↑doses required
TX: Thyroid hormone replacement |
|
|
Term
|
Definition
Endocrine (Thyroid)
MOA: Synthetic T3, binds to specific nuclear receptor to regulate transcription of specific genes
Prim EFF: ↑O2 Consumption, BMR; ↑lipolysis, glycogenolysis, gluconeogenesis: ↓cholesterol synthesis; ↑β-adrenergic responsiveness; ↑cardiac contractility, rate of contraction, cardiac output; ↑turnover of hormones, drugs; ↑bone turnover
SE:
Nervousness, arrhythmia, HTN,
SOB, N/V, diarrhea, heat intolerance,
↓reproductive fx; Higher activity = greater risk of cardiotoxicity
OTHER: Use limited: rapid absorption & shorter T1/2 → spiking, uneven blood levels, transient action
TX: i.v. for myxedema coma Oral tablets used primarily for short term suppression of TSH |
|
|
Term
|
Definition
Endocrine (thyroid)
MOA: Inhibit thyroid peroxidase →
↓TH synthesis
Propyl: Preggos
Methim: longer duration
SE: Rash, agranulocytosis, arthralgia,
myalgia, hepatic necrosis (P),
cholestatic jaundice (M)
OTHER: Propylthiouracil ↓T4→T3 conversion
TX: Graves disease
Thyrotoxicosis |
|
|
Term
|
Definition
Endocrine (Thyroid)
Inhibit thyroid peroxidase →
↓TH synthesis
Propyl: Preggos
Methim: longer duration
SE: Rash, agranulocytosis, arthralgia,
myalgia, hepatic necrosis (P),
cholestatic jaundice (M)
Propylthiouracil ↓T4→T3 conversion
TX: Graves disease
Thyrotoxicosis |
|
|
Term
|
Definition
Endocrine (Thyroid)
Selectively destroys thyroid tissue
Coadmin: β-blockers or Ca2+
channel blockers for Sx SE: Hypothyroidism OTHER: Doesn't increase cancer risk or
fertility or effect offspring
Hyperthyroidism |
|
|
Term
|
Definition
Endocrine (Calcium Homeostasis)
Bisphosphonates (pyroPO4 analogs)
Bind OH-apatite → ↓osteoclasts
↑bone mass
Absorbed IV much better than PO
PO: take w/full glass of water
SE: Hypocalcemia, hypophosphatemia
Upper GI distress
TX: Paget's Dz
Osteoporosis
Malignancy ↑Ca2+ |
|
|
Term
|
Definition
Endocrine (Calcium Homeostasis)
Bisphosphonates (pyroPO4 analogs)
Bind OH-apatite → ↓osteoclasts
↑bone mass
Absorbed IV much better than PO
PO: take w/full glass of water
SE: Hypocalcemia, hypophosphatemia
Upper GI distress
TX: Paget's Dz
Osteoporosis
Malignancy ↑Ca2+ |
|
|
Term
|
Definition
Endocrine (Calcium Homeostasis)
Bisphosphonates (pyroPO4 analogs)
Bind OH-apatite → ↓osteoclasts
↑bone mass
Absorbed IV much better than PO
PO: take w/full glass of water
SE: Hypocalcemia, hypophosphatemia
Upper GI distress
TX: Paget's Dz
Osteoporosis
Malignancy ↑Ca2+ |
|
|
Term
|
Definition
Endocrine (Calcium Homeostasis)
Binds calcitonin receptors → ↑cAMP
→ ↓osteoclast-mediated Ca2+
mobilization & ↑ excretion
SE: Nausea, facial flushing, hand
swelling, urticaria, resistance
OTH: Salmon CT is ↑potent and ↑t1/2
20% develop resistance
TX: Hypercalcemia
HyperPTH, ↑VitD, Bone mets
Osteoporosis, Paget's Dz |
|
|
Term
|
Definition
Endocrine (Calcium Homeostasis)
Vitamine D
Binds VitD receptor + RXR →
↑calbindins & ↑osteocalcin &
↑osteoclast formation & ↑Ca2+
Stored for prolonged periods in fat SE: Hypervitaminosis D: hypercalcemia
TX: HypoPTH, pseudohypoPTH
Rickets, osteomalacia
Osteoporosis |
|
|
Term
|
Definition
Endocrine (Calcium Homeostasis)
Vitamin D Hormone Prep.
Binds VitD receptor + RXR →
↑calbindins & ↑osteocalcin &
↑osteoclast formation & ↑Ca2+
Stored for prolonged periods in fat SE: Hypervitaminosis D: hypercalcemia
TX: HypoPTH, pseudohypoPTH
Rickets, osteomalacia
Osteoporosis |
|
|
Term
|
Definition
Endocrine (Calcium Homeostasis)
PTH:
Binds PTH receptors → ↑Ca2+ bone
mobilization & ↑renal Mg & Ca (↓PO4)
reabsorption & ↑vit.D production
MET: Daily intermittent admin ↑osteoblasts
& bone formation
(not bone resorption!)
Not used to treat hypocalcemia
Hypoparathyroidism
TX: Dx pseudohyperPTH
Osteoporosis |
|
|
Term
| Cortisol (Hydrocortisone) |
|
Definition
| Endocrine (Glucocorticoids) Bind glucocorticoid receptors → ↑gluconeogenesis ↑glycogenesis ↑hormone-sensitive lipase ↑blood glucose ↓cytokines ↑vasoCX demarginalized PMNs ↓vitamin D → ↓Ca2+ absorption & ↑Ca2+ clearance & ↑bone resorption MET: Short-acting SE: ↑susceptibility to infx Inhibits growth in kids Myopathy Osteoporosis Cataracts Adrenocortical atrophy Iatrogenic Cushing's TX: Addison's disease |
|
|
Term
|
Definition
| Endocrine (Glucocorticoids) MOA: Bind glucocorticoid receptors → ↑gluconeogenesis ↑glycogenesis ↑hormone-sensitive lipase ↑blood glucose ↓cytokines ↑vasoCX demarginalized PMNs ↓vitamin D → ↓Ca2+ absorption & ↑Ca2+ clearance & ↑bone resorption MET: Long-acting 30x anti-inflammatory 10x topical SE: ↑susceptibility to infx Inhibits growth in kids Myopathy Osteoporosis Cataracts Adrenocortical atrophy Iatrogenic Cushing's TX: Dx of hypercortisolism Congenital adrenal hyperplasia |
|
|
Term
|
Definition
| Endocrine (Glucocorticoids) MOA: Bind glucocorticoid receptors → ↑gluconeogenesis ↑glycogenesis ↑hormone-sensitive lipase ↑blood glucose ↓cytokines ↑vasoCX demarginalized PMNs ↓vitamin D → ↓Ca2+ absorption & ↑Ca2+ clearance & ↑bone resorption MET: Short-acting 4x anti-inflammatory SE: ↑susceptibility to infx Inhibits growth in kids Myopathy Osteoporosis Cataracts Adrenocortical atrophy Iatrogenic Cushing's TX: Addison's disease |
|
|
Term
|
Definition
Endocrine (Glucocorticoids)
MOA:
Bind glucocorticoid receptors →
↑gluconeogenesis
↑glycogenesis
↑hormone-sensitive lipase
↑blood glucose
↓cytokines
↑vasoCX
demarginalized PMNs
↓vitamin D → ↓Ca2+ absorption &
↑Ca2+ clearance & ↑bone resorption
MET: Short-acting
4x anti-inflammatory
SE:
↑susceptibility to infx
Inhibits growth in kids
Myopathy
Osteoporosis
Cataracts
Adrenocortical atrophy
Iatrogenic Cushing's
TX: Addison's disease |
|
|
Term
|
Definition
Endocrine (Glucocorticoids)
MOA:
Bind glucocorticoid receptors →
↑gluconeogenesis
↑glycogenesis
↑hormone-sensitive lipase
↑blood glucose
↓cytokines
↑vasoCX
demarginalized PMNs
↓vitamin D → ↓Ca2+ absorption &
↑Ca2+ clearance & ↑bone resorption
MET: Intermediate-acting
5x anti-inflammatory
5x topical
SE:
↑susceptibility to infx
Inhibits growth in kids
Myopathy
Osteoporosis
Cataracts
Adrenocortical atrophy
Iatrogenic Cushing's
TX: Addison's Disease |
|
|
Term
|
Definition
Endocrine (Mineralocorticoid)
MOA: Acts on renal DCT & CT cells to increase reabsorption of sodium, bicarbonate, and water in exchange for potassium
SE: Hypokalemia, CHF due to volume overload
TX: Replacement therapy after adrenalectomy or for primary and secondary adrenocortical insufficiency |
|
|
Term
|
Definition
| Endocrine (Mineralocortoid) MOA: Binds mineralocorticoid receptor → ↑Na+ reabs. & ↑K+ secretion SE: Hypernatremia, hypokalemia Metabolic alkalosis, hypervolemia Hypertension TX: Primary adrenocortical deficiency |
|
|
Term
|
Definition
| Endocrine (Mineralocorticoid Rec Antag) Competitive mineralocorticoid receptor antagonist; androgen receptor antagonist; inhibits 17α-Hydroxylase (in treatment of hirsutism) TX: Primary hyperaldosteronism; hirsutism |
|
|
Term
|
Definition
Endocrine (Androgens)
MOA: Anabolic - increase in overall body growth, muscle mass, and red blood cell production. Androgenic - growth of the larynx and skeleton, development of facial hair, darkening of the skin
MET: Sig. first pass metabolism; IV or IM best. Oral agents more hepatotoxic and less effective
SE: Behavioral effects - excessive rage or hostility; Increased LDL/HDL ratio; Stunted growth due to premature closure of the epiphyseal plates; Women - hirsutism, depression of menss, acne, and clitoral enlargement; Males - decreased spermatogenesis, gynecomastia, acne, testicular atrophy, prostatic hypertrophy
TX: Replacement therapy in male hypogonadism. Growth in pre-pubertal boys |
|
|
Term
|
Definition
Endocrine (Androgens)
Esterified Testosterone Der.
MOA: Anabolic - increase in overall body growth, muscle mass, and red blood cell production. Androgenic - growth of the larynx and skeleton, development of facial hair, darkening of the skin
MET: IM depot every 2 weeks
SE: Behavioral effects - excessive rage or hostility; Increased LDL/HDL ratio; Stunted growth due to premature closure of the epiphyseal plates; Women - hirsutism, depression of menss, acne, and clitoral enlargement; Males - decreased spermatogenesis, gynecomastia, acne, testicular atrophy, prostatic hypertrophy
TX: Replacement therapy in male hypogonadism. Growth in pre-pubertal boys |
|
|
Term
|
Definition
Endocrine (Androgens)
17α-alkylated derivative
MOA: Anabolic - increase in overall body growth, muscle mass, and red blood cell production. Androgenic - growth of the larynx and skeleton, development of facial hair, darkening of the skin
MET: Alkylated Oral preparation; More hepatotoxic
SE: Behavioral effects - excessive rage or hostility; Increased LDL/HDL ratio; Stunted growth due to premature closure of the epiphyseal plates; Women - hirsutism, depression of menss, acne, and clitoral enlargement; Males - decreased spermatogenesis, gynecomastia, acne, testicular atrophy, prostatic hypertrophy
TX: Replacement therapy in male hypogonadism. Growth in pre-pubertal boys |
|
|
Term
|
Definition
Endocrine (Androgens)
17α-alkylated derivative
MOA: Anabolic - increase in overall body growth, muscle mass, and red blood cell production. Androgenic - growth of the larynx and skeleton, development of facial hair, darkening of the skin
MET: Alkylated Oral preparation; More hepatotoxic
SE: Behavioral effects - excessive rage or hostility; Increased LDL/HDL ratio; Stunted growth due to premature closure of the epiphyseal plates; Women - hirsutism, depression of menss, acne, and clitoral enlargement; Males - decreased spermatogenesis, gynecomastia, acne, testicular atrophy, prostatic hypertrophy
TX: Replacement therapy in male hypogonadism. Growth in pre-pubertal boys |
|
|
Term
|
Definition
Endocrine (Androgens)
17α-alkylated derivative
MOA: Anabolic - increase in overall body growth, muscle mass, and red blood cell production. Androgenic - growth of the larynx and skeleton, development of facial hair, darkening of the skin
MET: Alkylated Oral preparation; More hepatotoxic
SE: Behavioral effects - excessive rage or hostility; Increased LDL/HDL ratio; Stunted growth due to premature closure of the epiphyseal plates; Women - hirsutism, depression of menss, acne, and clitoral enlargement; Males - decreased spermatogenesis, gynecomastia, acne, testicular atrophy, prostatic hypertrophy
TX: Replacement therapy in male hypogonadism. Growth in pre-pubertal boys |
|
|
Term
|
Definition
Endocrine (Nonsteroidal Comp. Antag. to Androgen Rec.)
MOA: Converted to dihydroxyflutamide →
blocks DHT binding to receptors; Used with GnRH agonist
SE: GI Distress
TX: Prostate cancer |
|
|
Term
| Testosterone/Epitestosterone |
|
Definition
Endocrine (Anabolic Steroids)
Giving Testosterone with Epitestosterone keeps the ratio 1:1 and is harder to detect than if just testosterone is given. (tests check ratio not absolute amounts) |
|
|
Term
|
Definition
Endocrine (Anabolic Steroids)
THG "Designer Testosterone" produced to avoid earlier drug tests.
Admin: Cycling, Stacking, Pyramiding
SE: Retention of Na/H2O (↑vascular resistance, ↑blood volume, ↑hypertension); ↑risk of coronary heart disease (↓ HDL:↑LDL); Acne; Liver Toxicity (oral preps; blood cysts, ↑liver tests, tumors) |
|
|
Term
|
Definition
Endocrine (steroid syn inhibitors)
MOA: Blocks conversion of cholesterol → pregnenolone
Inhibits aromatase & desmolase →
↓ estradiol
TX: Breast cancer
(Post-men; in ER+ tumors)
SE: CNS depression
(drowsiness, blurry vision, ataxia)
OTH: Post-menopause women
produce estrogen in adrenal
cortex….. Medical
The breast way to treat
Tammy, Ethyl, Anna, and
Lenny is by aromatherapy. |
|
|
Term
|
Definition
| Endocrine (steroid syn inhibitors) MOA: partial agonist at PR, AR, and Glucocorticoid receptor; induces a hyperandrogenic state which induces atrophy of ectopic endometrial tissue and reduces pain (offset by androgenic SE) SE: Weight gain; Edema; Acne; ↓HDL TX: endometriosis |
|
|
Term
|
Definition
| Endocrine (steroid syn inhibitors) MOA: steroidal irreversible inhibitor of aromatase (inhibits testosterone → estrogen) SE: Nausea, fatigue, & hot flashes TX: Advanced breast cancer in postmenopausal women which has progressed after Tamoxifen therapy |
|
|
Term
|
Definition
Endocrine (steroid syn inhibitor)
MOA: Blocks 5α-reductase → inhibits
conversion of testosterone → DHT
Admin: oral
SE: ↓libido
Ejaculation disorders
Eretctile dysfunction
Pregnant women should not be
exposed (hypospadias)
TX: Androgenic alopecia; Benign prostatic hyperplasia (BPH) |
|
|
Term
|
Definition
Endocrine (steroid syn inhibitor)
MOA: inhibits several of the cytochrome P-450 enzymes involved in steroid synthesis
TX: Cushing's syndrome |
|
|
Term
|
Definition
Endocrine (steroid syn inhibitor)
Blocks cortisol synthesis
TX: Cushing's syndrome |
|
|
Term
|
Definition
Endocrine
MOA: Zinc insulin crystals in a neutral,
unbuffered suspension
MET: Short-acting
Admin: IV or subQ
(30-60 min before meal)
SE:
Hypoglycemia
(Counter-reg. often impaired)
Mild: juice/glucose
Severe: glucagon
~
Allergy
(insulin or protamine)
~
Insulin resistance (IgG)
~
Lipohypertrophy
OTH:
Insulin requirements ↑ during 2nd
half of pregnancy
~
If impaired renal fx: ↓insulin
clearance
TX:
Type 1 diabetes |
|
|
Term
|
Definition
Endocrine
MOA: 30% semilente insulin + 70%
ultralente insulin crystals in acetate
buffer
METAB: Intermediate-acting
SE:
Hypoglycemia
(Counter-reg. often impaired)
Mild: juice/glucose
Severe: glucagon
~
Allergy
(insulin or protamine)
~
Insulin resistance (IgG)
~
Lipohypertrophy
TX: Type 1 DM |
|
|
Term
|
Definition
Endocrine
MOA: Insulin(-) complexed w/protamine(+)
& zinc
MET: Intermediate-acting
SE:
Hypoglycemia
(Counter-reg. often impaired)
Mild: juice/glucose
Severe: glucagon
~
Allergy
(insulin or protamine)
~
Insulin resistance (IgG)
~
Lipohypertrophy
OTH:
Insulin requirements ↑ during 2nd
half of pregnancy
~
If impaired renal fx: ↓insulin
clearance
TX:
Type 1 diabetes |
|
|
Term
|
Definition
Endocrine
MOA: Excess zinc (produces large
crystals) in acetate buffer
MET: Long-acting
SE:
Hypoglycemia
(Counter-reg. often impaired)
Mild: juice/glucose
Severe: glucagon
~
Allergy
(insulin or protamine)
~
Insulin resistance (IgG)
~
Lipohypertrophy
OTH:
Insulin requirements ↑ during 2nd
half of pregnancy
~
If impaired renal fx: ↓insulin
clearance
TX: Type 1 Diabetes |
|
|
Term
|
Definition
Endocrine
MOA: Peakless recombinant insulin that
precipitates in neutral subQ tissues
MET: Ultra-long-acting
Delayed onset of action
SE:
Hypoglycemia
Counter-reg. often impaired)
Mild: juice/glucose
Severe: glucagon
~
Allergy
(insulin or protamine)
~
Insulin resistance (IgG)
~
Lipohypertrophy
OTH:
Insulin requirements ↑ during 2nd
half of pregnancy
~
If impaired renal fx: ↓insulin
clearance
TX:
ype 1 diabetes |
|
|
Term
|
Definition
Endocrine
MOA: Able to stay as monomer, because
proline & lysine AA's are swapped
MET: Ultra-fast & short-acting
SE:
Hypoglycemia
Counter-reg. often impaired)
Mild: juice/glucose
Severe: glucagon
~
Allergy
(insulin or protamine)
~
Insulin resistance (IgG)
~
Lipohypertrophy
OTH:
Insulin requirements ↑ during 2nd
half of pregnancy
~
If impaired renal fx: ↓insulin
clearance
TX: Type 1 Diabetes |
|
|
Term
|
Definition
| Endocrine (GLP-1 analogue peptide) MOA: Glucagon-like peptide agonist → ↓gastric emptying & ↓post-pran glucagon & ↑insulin secretion MET: GLP-1 secreted in response to food to potentiate glucose-stim insulin release SE: N/V, diarrhea Contraind: hypersensitivity, gastroparesis, hypoglycemia unawareness TX: Type 2 diabetes |
|
|
Term
|
Definition
| Endocrine (Amylin analogue) MOA: Amylin analog → ↓gastric emptying & ↑satiety & ↓post-pran glucagon Admin: subQ w/mealtime insulin Don't use w/acarbose SE: ↑Insulin-induced severe hypoglycemia Contraind: hypersensitivity, gastroparesis, hypoglycemia unawareness TX: Type 1 diabetes Type 2 diabetes |
|
|
Term
|
Definition
| Endocrine (α-glucosidase inh.) MOA: Competitive α-glucosidase inhibitors → ↓carbohydrate digestion/absorb Blunted post-prandial glucose MET: Low systemic bioavailability Taken with a meal SE: Flatulence, nausea, diarrhea Contraind: IBS, obstruction, ulcer OTH: Do not cause hypoglycemia, lactic acidosis, or weight gain TX: Type 2 diabetes |
|
|
Term
|
Definition
| Endocrine (Biguanide) MOA: ↓ gluconeogenesis ↑insulin-stimulated GLUT4 trafficking to membrane ↑cAMP-act. protein kinase (Increase tissue sensitivity to insulin) MET: Not significantly metabolized 90% oral dose gone in 24 hours Half-life: 2 hours Low potency SE: Lactic acidosis (Even less with 2nd generation) Cardiovascular disorders OTH: Do not cause hypoglycemia (even at high doses) ↓TAG, ↓cholesterol, ↓LDL, ↑HDL Weight loss & ↓BP TX: DOC Type 2 Diabetes (Obese) |
|
|
Term
|
Definition
Endocrine (Dipeptidase 4 Inhibitor)
MOA: Blocks dipeptidyl peptidase IV →
↓GLP-1 & GIP → ↑post-pran insulin
MET: With: diet & exercise
With: metformin or TZD
TX: Type 2 diabetes |
|
|
Term
|
Definition
Endocrine (Sulfonylureas)
MOA: Bind SUR receptors associated w/
ATP-sensitive K+ channels →
↓K+ current → ↑insulin secretion
MET: Once daily dosing
SE:
Severe hypoglycemia
(chlorpropamide & glyburide)
Weight gain
Skin reactions & erythema
Blood dyscrasias
Hepatic dysfunction
(All are liver metabolized)
GI disturbances
OTH: Does not cross placenta
(can use for gestational diabetes)
TX: Type 2 diabetes |
|
|
Term
|
Definition
Endocrine (Sulfonylureas)
MOA: Bind SUR receptors associated w/
ATP-sensitive K+ channels →
↓K+ current → ↑insulin secretion
MET: Second generation
SE:
Severe hypoglycemia
(chlorpropamide & glyburide)
Weight gain
Skin reactions & erythema
Blood dyscrasias
Hepatic dysfunction
(All are liver metabolized)
GI disturbances
OTH: Extended release form does not
induce weight gain!
TX: Type 2 Diabetes |
|
|
Term
|
Definition
Endocrine (Meglitinides)
MOA: Bind SUR receptors associated w/
ATP-sensitive K+ channels (diff. site
from sulfonylureas) → ↓K+ current
→ ↑insulin secretion
MET: Metabolized by liver
Half-life: even shorter & rapider (than SUR and Repaglinide)
SE:
Hypoglycemia
Weight gain
OTH:
Used for post-pran hyperglycemia
TX: Type 2 diabetes |
|
|
Term
|
Definition
Endocrine (Meglitinides)
MOA: Bind SUR receptors associated w/
ATP-sensitive K+ channels (diff. site
from sulfonylureas) → ↓K+ current
→ ↑insulin secretion
MET: Metabolized by liver
Half-life: 1 hour
SE:
Hypoglycemia
Weight gain
OTH:
Used for post-pran hyperglycemia
TX: Type 2 diabetes |
|
|
Term
|
Definition
Endocrine (Thiazolidinediones)
MOA: Bind PPAR-γ receptor + RXR →
↑GLUT1 & GLUT4
↑lipoprotein lipase, FABPaP2
↓TNFα, ↓leptin
MET: Metabolized to weak metabolites
Half-life: 3-7 hours
↑albumin bound
SE:
Troglitazone: hepatotoxicity
Heart failure
Angina, MI
OTH: Dep on presence of insulin for their activity.
Do not cause hypoglycemia
Current TZD's do not cause
hepatotoxicity
TX:
Type 2 diabetes |
|
|
Term
|
Definition
Endocrine (Thiazolidinediones)
MOA: Bind PPAR-γ receptor + RXR →
↑GLUT1 & GLUT4
↑lipoprotein lipase, FABPaP2
↓TNFα, ↓leptin
MET: Metabolized to inactive metabolites
Half-life: 3-4 hours
↑albumin bound
SE:
Troglitazone: hepatotoxicity
Heart failure
Angina, MI
OTH:
Do not cause hypoglycemia
Current TZD's do not cause
hepatotoxicity
TX: Type 2 Diabetes |
|
|
Term
|
Definition
| Endocrine (Hyperglycemics) MOA: ↑ open time of ATP-sensitive K+ channel → ↓insulin release MET: Metabolized in liver Half-life: 48 hours SE: Nausea/vomiting Fluid & salt retention OTH: Does not inhibit the synthesis of insulin, only the release TX: Insulinoma |
|
|
Term
|
Definition
Endocrine (Hyperglycemics)
MOA: Binds glucagon receptor → ↑cAMP
→ ↑(P) glycogen phosphorylase &
synthase
Admin: subQ, IM, IV
Half-life: 3-6 minutes
Metabolism: 25% first-pass
SE: Nausea & vomiting
OTH: Inotropic & chronotropic
RX of GI smooth muscle
Release catecholamines & CT
TX:
Severe hypoglycemia
Shock & GI RX
Dx pheochr-cytoma |
|
|
Term
|
Definition
Hypolipidemics (bile-acid sequesterant)
MOA:
(+) charged resins that bind bile
acids → ↓reabsorption of bile acids
→ ↓cholesterol & ↑LDL receptors
MET: Taken with meals PO
SE: HyperTAG
GI (constipation) Impeded absorption of Fat-soluble Vitamins and Drugs
OTH: Negligible systemic bioavailability
Approved for use in children
TX: Familial HyperTAG
FC hyperTAG |
|
|
Term
|
Definition
Hypolipidemics (bile-acid sequesterant)
MOA: (+) charged resins that bind bile
acids → ↓reabsorption of bile acids
→ ↓cholesterol & ↑LDL receptors
MET: Taken with meals PO
SE: HyperTAG
GI (constipation) Impeded absorption of Fat-soluble Vitamins and Drugs
OTH: Negligible systemic bioavailability
Approved for use in children
TX: Familial HyperTAG
FC hyperTAG |
|
|
Term
|
Definition
Hypolipidemics (cholesterol absorption inhibitor)
MOA: ↓cholesterol transport at brush
border in small intestine lumen →
↓cholesterol & ↓LDL-C & ↑HDL
MET: Enterohepatic recycling
Half-life: 22 hours
Low systemic bioavailability
OTH: Cholesterol lowering effect limited
by ↑liver cholesterol synthesis
TX: Hypercholesterolemia |
|
|
Term
|
Definition
Hypolipidemics (fibrates -TG)
MOA:
Bind PPAR-α+ RXR → ↓apoC-III &
apoB & ↑lipoprotein lipase → ↓VLDL
→ ↓LDL & ↑apoA
MET: Half-life: 1.5 hours
Highly albumin bound
SE:
GI disturbances
Rash, myopathy, arrhythmia
Fatigue
TX: HyperTAG
Dysbetalipoproteinemia
FC hyperTAG |
|
|
Term
|
Definition
Hypolipidemics (fibrates -TG)
MOA:
Bind PPAR-α+ RXR → ↓apoC-III &
apoB & ↑lipoprotein lipase → ↓VLDL
→ ↓LDL & ↑apoA
MET: Half-life: 1.5 hours
Highly albumin bound
SE:
GI disturbances
Rash, myopathy, arrhythmia
Fatigue
TX: HyperTAG
Dysbetalipoproteinemia
FC hyperTAG |
|
|
Term
|
Definition
Hypolipidemics (fibrates -TG)
MOA:
Bind PPAR-α+ RXR → ↓apoC-III &
apoB & ↑lipoprotein lipase → ↓VLDL
→ ↓LDL & ↑apoA
MET: Half-life: 1.5 hours
Highly albumin bound
SE:
GI disturbances
Rash, myopathy, arrhythmia
Fatigue
TX: HyperTAG
Dysbetalipoproteinemia
FC hyperTAG |
|
|
Term
|
Definition
Hypolipedemics (HMG-Coa Reductase inhib)
MOA: Inhibit HMG CoA reductase (HMG
CoA → mevalonate) → ↓cholesterol
& ↑LDL receptors
MET: First pass metabolism
Cytochrome P450 metabolized
Extensively protein bound
SE:
Myopathy (↑CK)
Renal dysfx (myoglobinuria)
Rhabdomyolysis (w/gemfribrozil)
OTH:
↑BMP-2 → ↑osteoblasts →
↓fracture risk
TX: Hypercholesterolemia
(& familial) |
|
|
Term
|
Definition
Hypercholesterolemia
(& familial) |
|
|
Term
|
Definition
Hypercholesterolemia
(& familial) |
|
|
Term
|
Definition
| Hypolipidemic MOA: Vitamin B3 → ↓hepatic TAG synthesis & ↑lipoprotein lipase → ↓apoB → ↓VLDL → ↓LDL MET: Half-life: 1 hour Used w/: bile acid binding resin Used w/: HMG CoA reductase inh. SE: Flushing, pruritis Nausea, diarrhea, peptic ulcer Hepatotoxic, glucose intol., gout OTH: Most effective agent to ↑HDL Only agnet to ↓Lp(a) TX: HyperTAG Familial hyperTAG FC hyperTAG |
|
|
Term
|
Definition
| Weight Loss MOA: Amphetamine derivative Inhibits NE reuptake Coadmin: fenfluramine (Pulmonary HTN & valve problems) Interax: MAOI, guaneth, stim, EtOH, sibutramine, TCA SE: Drug mouth, insomnia, constipation, ↑BP, ↑HR, abuse OTH: Fenfluramine releases 5-HT & inhibits 5-HT reputake Contraind: hyperthyroid, HTN, CVD, glaucoma, anxiety TX: Obesity |
|
|
Term
|
Definition
| Weight Loss MOA: Inhibit NE reuptake Coadmin: fenfluramine (Pulmonary HTN & valve problems) Interax: MAOI, guaneth, stim, EtOH, sibutramine, TCA SE: Drug mouth, insomnia, constipation, ↑BP, ↑HR, abuse OTH: Fenfluramine releases 5-HT & inhibits 5-HT reputake Contraind: hyperthyroid, HTN, CVD, glaucoma, anxiety TX: Obesity |
|
|
Term
|
Definition
Weight Loss
MOA: Inhibits NE, 5-HT, DA reuptake
Interax: MAOI, SSRI, triptans,
ergotamines, dextromethorphan,
opioids, lithium, tryptophan
SE: Drug mouth, insomnia, constipation,
↑BP, ↑HR, abuse
OTH: Lose 10-15% of weight
Contraind: HTN, renal/liver impair,
addx, CAD, CHF, arrhythmia, stroke
TX: Obesity |
|
|
Term
|
Definition
| Weight Loss MOA: Inhibits GI lipases → ↓dietary fat absorption Interax: cyclosporine SE: Gas, oily stools, ↑defecation ↓absorption of ADEK & β-carotene OTH: Lose 8-10% of weight Improves H1Ac & sulfonylurea dose Contraind: malabsorption, cholestitis TX: Obesity |
|
|
Term
|
Definition
| Appetite Stimulant MOA: Cannabinoid CB1, CB2 receptor partial agonist TX: anti-emetic, appetite stimulant, mild analgesic(?) |
|
|
Term
|
Definition
Asthma
MOA:
β2-agonists → Gs → ↑cAMP →
bronchoRX
Admin: Metered dose inhaler
Nebulizers
SE:
Anxiety, tremor, restlessness, ↑HR,
hypokalemia
OTH: Albuterol is the most used
Metered dose inhaler is most
common
TX:
Acute asthma attack |
|
|
Term
|
Definition
Asthma
MOA: β2-agonists → Gs → ↑cAMP →
bronchoRX
Admin: Metered dose inhaler
Nebulizers
SE:
Anxiety, tremor, restlessness, ↑HR,
hypokalemia
OTH: Albuterol is the most used
Metered dose inhaler is most
common
TX:
Acute asthma attack |
|
|
Term
|
Definition
Asthma
MOA:
β2-agonists → Gs → ↑cAMP →
bronchoRX
MET: Long-acting
Salmeterol = slow-acting
Formoterol = fast-acting
SE: Salmeterol is not useful in acute
asthma attacks!
(Slow onset of action)
TX:
Severe refract asthma
COPD
Chronic bronchitis |
|
|
Term
|
Definition
Asthma
MOA:
β2-agonists → Gs → ↑cAMP →
bronchoRX
MET: Long-acting
Salmeterol = slow-acting
Formoterol = fast-acting
SE: Salmeterol is not useful in acute
asthma attacks!
(Slow onset of action)
TX:
Severe refract asthma
COPD
Chronic bronchitis |
|
|
Term
|
Definition
Asthma (Glucocorticoid)
MOA:
Inhibit late-phase reactions of
inflammation
Decrease bronchial reactivity
Most potent anti-asthma agents
available
Admin: inhalation
SE: Budesonide Less active at hypothalamic-pituitary-adreno axis;
Systemic corticosteroid effects
Hoarseness
Oropharyngeal candidiasis
Coughing, wheezing
HPA axis suppression
Long-term therapy (>3weeks) only if
refractory to other trx
TX: Acute asthma |
|
|
Term
|
Definition
Asthma (Glucocorticoid)
MOA:
Inhibit late-phase reactions of
inflammation
Decrease bronchial reactivity
Most potent anti-asthma agents
available
Admin: inhalation
SE: Budesonide Less active at hypothalamic-pituitary-adreno axis;
Systemic corticosteroid effects
Hoarseness
Oropharyngeal candidiasis
Coughing, wheezing
HPA axis suppression
Long-term therapy (>3weeks) only if
refractory to other trx
TX: Acute asthma |
|
|
Term
|
Definition
Asthma (Glucocorticoid)
MOA:
Inhibit late-phase reactions of
inflammation
Decrease bronchial reactivity
Most potent anti-asthma agents
available
Admin: inhalation
SE: Budesonide Less active at hypothalamic-pituitary-adreno axis;
Systemic corticosteroid effects
Hoarseness
Oropharyngeal candidiasis
Coughing, wheezing
HPA axis suppression
Long-term therapy (>3weeks) only if
refractory to other trx
TX: Acute asthma |
|
|
Term
|
Definition
Asthma (Glucocorticoid)
MOA:
Inhibit late-phase reactions of
inflammation
Decrease bronchial reactivity
Most potent anti-asthma agents
available
Admin: inhalation
SE: Budesonide Less active at hypothalamic-pituitary-adreno axis;
Systemic corticosteroid effects
Hoarseness
Oropharyngeal candidiasis
Coughing, wheezing
HPA axis suppression
Long-term therapy (>3weeks) only if
refractory to other trx
TX: Acute asthma |
|
|
Term
|
Definition
| Asthma (mAch-antag) MOA: mACh receptor antagonist → ↓Gi → ↑cAMP & ↓PLC → bronchoRX Admin: dry powder inhalation TX: Chronic bronchitis Limited in asthma |
|
|
Term
|
Definition
Asthma (mAch-antag)
MOA: mACh receptor antagonist → ↓Gi →
↑cAMP & ↓PLC → bronchoRX
Admin: dry powder inhalation
TX: Chronic bronchitis
Limited in asthma |
|
|
Term
|
Definition
Asthma (LTD4 leukotriene antag)
MOA: Weak anti-inflammatory &
bronchodilator actions
MET: Best if added to ICS therapy
(allows lower doses)
SE: rarely, vasculitis and systemic eosinophilia
TX: Asthma
(maintenance) |
|
|
Term
|
Definition
Asthma (LTD4 leukotriene antag)
MOA: Weak anti-inflammatory &
bronchodilator actions
MET: Best if added to ICS therapy
(allows lower doses)
SE: rarely, vasculitis and systemic eosinophilia
TX: Asthma
(maintenance) |
|
|
Term
|
Definition
Asthma (antibodies)
MOA: Monoclonal anti-IgE antibody
OTH: Allowed lower doses of ICS &
↓hospitalizations & ER visits
TX: Asthma
(maintenance) |
|
|
Term
|
Definition
Asthma (preventative)
MOA: Prevents mast cell degranulation
(asthma prophylaxis)
Admin: metered dose inhaler
Spinhaler
4x day regimen
SE:
Virtually no side effects
OTH: No role in acute asthma!
TX:
Asthma
(maintenance) |
|
|
Term
|
Definition
Asthma (preventative)
MOA: Prevents mast cell degranulation
(asthma prophylaxis)
Admin: metered dose inhaler
Spinhaler
4x day regimen
SE:
Virtually no side effects
OTH: Greater potency than cromolyn
Additive therapeutic effects with
corticosteroids
TX:
Asthma
(maintenance) |
|
|
Term
|
Definition
Malaria
MOA: Schizonticide → terminates fever &
parasitemia
Buildup of free heme
MET:
Resistance: mutant PfCRT trx
(reversed by verapamil & desipramine)
SE:
Pruritus, nausea, anorexia, blurring
Hemolysis in G6PD, Wide QRS
AGRANULOCYTOSIS, oto/retinopathy
OTH:
Does not eliminate liver forms
(P. vivax & P. ovale)
No P. falciparum gametocyte kill
TX: PF malaria
Hepatic amebic abscess |
|
|
Term
|
Definition
Malaria
MOA:
Unknown
MET: Metabolized by liver, excreted by kidney
Coadmin: doxycycline
Only used in chloroquin-resistant
SE:
Cardiotoxicity, hematologic
Cinchonism, hypersensitivity
Blackwater fever, ↓glucose, uteroCX
OTH:
Does not eliminate liver forms
(P. vivax & P. ovale)
No P. falciparum gametocyte kill
TX: PF malaria |
|
|
Term
|
Definition
Malaria
MOA: Schizonticide
Used as prophylaxis
MET:
Long half-life (~20 days)
SE: GI
Neuropsychiatric
Cardiac & blood dyscrasias
OTH:
Does not eliminate liver forms
(P. vivax & P. ovale)
No P. falciparum gametocyte kill
TX:
PF malaria
(chloroquine resistant) |
|
|
Term
|
Definition
Malaria
MOA: Synthetic 8-aminiquinoline
MET: Absorbed GI
Half-life: 3-8 hours
SE:
GI, methemoglobinemia
Hemolysis in G6PD
Cardiac & blood dyscrasias
OTH:
Only agent active against dormant
hypnozoite liver form
(P. vivax & P. ovale)
TX: Malaria |
|
|
Term
|
Definition
Malaria (folate inhib)
MOA: Active against RBC forms
Inhibit DHF reductase → ↓folate
Coadmin: sulfa drugs
(inh. DHP synthase = synergy)
SE: GI
Pruritus
TX: Malaria (p. falciparum) |
|
|
Term
|
Definition
Malaria (Sulfonamide)
MOA: Blockade of folic acid synthesis
Admin: used w/ Pyrimethamine (also folate inh)
TX: Malaria (chloroquine-res. P. falciparum) |
|
|
Term
|
Definition
Parasites (Trypanosomiasis T. brucei)
MOA: inhibition of enzymes involved in energy metabolism
Admin: IV
Does not cross BBB
SE:
GI
Neurological
Cardiovascular, blood dyscrasias
OTH:
Adding pentamidine may increase
efficacy
TX: Early hemolymphatic
African trypanosomiasis (T. brucei gambiense/rhodesiense) |
|
|
Term
|
Definition
Parasites (Trypanosomiasis T brucei)
MOA: Trivalent arsenical compound, inhibits sulfhydryl groups in parasite enzymes
Admin: IV
Does cross BBB
SE:
Reactive encephalopathy
Renal & cardiac toxicity
Hypersensitivity Hemolytic anemia (G6PD def)
TX: DOC CNS advanced African trypanosomiasis (T. brucei gambiense/rhodesiense) |
|
|
Term
|
Definition
Parasites (Trypanosomiasis)
MOA: Inhibits ornithine decarboxylase → blocks
conversion of ornithine → putrescine
Admin: IV
SE: GI
Blood dyscrasias
OTH:
Mammalian OC enzyme very short
half-life…trypanosome OC enzyme
much more stable
TX: CNS advanced
African trypanosomiasis (T. brucei gambiense/rhodesiense) |
|
|
Term
|
Definition
Parasites (Trypanosomiasis T. cruzi)
MOA: Forms intracellular oxygen radicals
Admin: oral
SE: GI
CNS Icterus Suppression of cell-mediated immunity
TX: Acute American
trypanosomiasis (T. cruzi) |
|
|
Term
|
Definition
Parasites (Leishmaniasis)
MOA: inhibition of glycolysis at the phosphofructokinase reaction
Admin: IM or IV
(daily)
SE:
GI
Fever, arthralgias
T wave changes, QT prolong
OTH: First line therapy
TX: Cutaneous & visceral
leishmaniasis (f/ sandflies) |
|
|
Term
|
Definition
Parasites (Amebiasis)
MOA: Causes multiple-strand breaks, disruption of
DNA replication & trx & inhibits DNA repair
Admin: oral
SE: Nausea, headache, metallic taste
GI, CNS, hematologic
Disulfiram-like reaction TERATOGENIC
OTH: May potentiate oral anticoagulants
TX: Giardiasis
Entamebiasis
Trichomoniasis (also G. vaginalis, B. fragilis, C. difficile) |
|
|
Term
|
Definition
Parasites (Belantidiasis)
MOA: antibiotic that eliminates the normal intestinal flora and therefore the ameba's main food source; direct killing of Balantidium coli (blocks aminoacyl tRNA)
MET: Dairy foods and antacids with magnesium and aluminum chelate the drug, low abs.
SE: Nausea
Photosensitivity
Can discolor teeth
(not given to children or pregnant)
TX: Ricketsia, M. pneumoniae, Chlamydia, Balantidia coli; indirect amebicide. |
|
|
Term
| Trimethaprim sulfamethoxazole |
|
Definition
Parasites (Pneumocystis carinii)
MOA: Dihydrofolate reductase inhibitor, stops conversion of dihydrofolate to tetrahydrofolate.
Admin: PO
SE: Rash, Dermatitis, Urticaria (esp. AIDS pts.) Stevens-Johnson syndrome GI Agranulocytosis, megaloblastic anemia (folate def. pts.), hemolytic anemia Headache Depression
OTH: most often combined with Sulfamethoxazole (sulfonamide - PABA analogue comp. inhibits dihydropteroate synthetase), synergistic
TX: UTI's Pneumonia (P. carinii) Bacterial prostatitis Salmonella Shigella Gonorrhea Sinusitis/bronchitis Acute otitis media Toxoplasmosis (2nd line) |
|
|
Term
|
Definition
Parasites (Pneumocystosis)
MOA: Effective against trypanosoma & P. carinii, high-affinity uptake system concentrates it, bind to organism's DNA or inhibit glycolysis
Admin: IM or IV
Half-life: ~6 hr
Accumulates in tissues (12 days)
SE:
Cardiovascular
Pancreatic, hepatic, renal, blood
Bronchospasm, dyspnea
OTH: Injectable (trypanosomatid)
Inhalation (pneumocystis)
TX: Trypanosomes (DOC T. brucei gambiense/rhodesiense hemolymphatic stage)
P. carinii |
|
|
Term
|
Definition
Parasites (Anti-Trematode/Cestode)
MOA: Isoquinoline-pyrazine derivative
↑cell membrane permeability to Ca2+ →
paralysis
Admin: oral
[↑]: cimetidine or carbs
[↓]: steroids or antiepileptics
SE:
Mild: headache, dizziness, GI,
myalgia, pruritis, fever
OTH: Bitter taste (don't chew)
TX: Schistosomiasis
Hydatid disease
Neurocysticercosis
Trematodes & Cestodes |
|
|
Term
|
Definition
Parasites (anti-cestodes)
MOA: Salicylamide derivative
Inhibits oxidative phosphorylation
Admin: oral
SE: Mild GI
OTH: no longer on US market; found to cause cysticercosis in pts infected with T. solium
TX: Cestodes (tapeworms) |
|
|
Term
|
Definition
Parasites (Cestodes)
MOA: Inhibits microtubule synthesis
Admin: oral
Poorly absorbed from GI
(effect ↑w/fatty meal)
SE:
Hypersensitivity reactions
Alopecia
OTH:
Wide-spectrum
TX: Ascariasis (roundworm)
Trichuriasis (whipworm)
Pin (E. vermicularis) & Hookworm (N. americanus) |
|
|
Term
|
Definition
Parasite (Cestodes)
MOA: Active albendazole sulfoxide, blocks glucose uptake
Admin: oral
Metabolized in liver to active form
SE:
Mild GI
Long-term use (hydatid):
↑liver enzyme & blood dyscrasia
OTH:
Admin fasting: luminal parasite
Admin fatty meal: tissue parasite
Coadmin: corticosteroids (cyst)
TX:
Cysticercosis (whipworm)
Hydatid disease
Round (Ascariasis), Pin (E. vermicularis), Hook (N. americanus) |
|
|
Term
|
Definition
Parasite (Nematode)
MOA: Tetrahydropyrimidine derivative
NMJ blocking agent → paralyzes & expels
Admin: oral
Poorly absorbed from GI (good!)
SE: GI
Insomnia
OTH: ACh release & AChE inhibition
Cure rates >90%
TX:
Ascariasis (roundworm)
Pinworm (Enterobius vermicularis)
Hookworm (Necator americanus) |
|
|
Term
|
Definition
Parasite (Nematode)
MOA: Direct GABA agonist
Blocks ACh at NMJ to produce nematode
flacid paralysis
Admin: oral
Excretion: w/in 24 hrs
SE: GI
OTH: Cure rate of ascariasis (>90%)
TX: Ascariasis (roundworm) |
|
|
Term
|
Definition
| RA (COX1 & COX2 Irreversible inh) Duration: Low = 15 min High = 4 h ↑ High = 13 h OTH: 1) binds serum proteins (depends on dose) 2) irreversibly acetylates COX-1&2, 3) irreversibly inhibits platelet aggregation SE: 1) salicylism, respirary alkalosis, met. acid 2) NSAID-asthma 3) Reyes syndome TX: Rheumatoid Arthritis, Inflammation |
|
|
Term
|
Definition
| RA (COX1 & COX2 Inh) MET: Liver CYP3A4 CYP2C9 Duration: Short (2hr) OTH: 1)↑ serum aminotransferase activity in liver 2) Renal dysfx doesn't impair clearance SE: Typical NSAID TX: Rheumatoid arthritis, Inflammation |
|
|
Term
|
Definition
| RA [Dolobid] (COX1 & COX2 Inh) MOA: Analgesia (low grade pain) Anti-pyretic (PG inhibition) Anti-inflamatory (MSK, RA, OA) Anti-coagulant (other NSAIDs can block long-lasting ASA) COX-2 Pro-coagulant (↓ COX-2 PGI but not COX-1 TXA) Duration: onset 1hr, analgesia 2-3 hr SE: GI irritation (ASA espclly) ↑ bleeding time (inhib. TXA) Kidney effects Pregnancy (delayed onset of labor from ↓ PGE & PGF) Hypersensitivity (↓ COX → arachidonate → ↑ lipoxygenase) TX: Rheumatoid Arthritis, Inflammation |
|
|
Term
|
Definition
| RA [Advil, Motrin] (COX1 & COX2 Inh) MET: Liver CYP2C8 Duration: Short (2hr) OTH: Low dose = analgesic (no anti-inflam) High dose = analgesic & anti-inflam SE: GI, rash, tinnitis, fluid retention kidney failure, hepatitis TX: RA, Chronic Inflammation |
|
|
Term
|
Definition
| RA [Indocid] (COX 1 & COX 2 Inh) OTH: Very potent indole derivative SE: 30% have to discontinue (psychosis & hallucination) TX: RA, Chronic Inflammation, Acute Gouty Attacks |
|
|
Term
|
Definition
| RA [Aleve] (COX1 & COX2 Inh) Duration: Long (12 hr) OTH: Free fraction is 40% higher in females SE: GI irritation (ASA espclly) ↑ bleeding time (inhib. TXA) Kidney effects Pregnancy (delayed onset of labor from ↓ PGE & PGF) Hypersensitivity (↓ COX → arachidonate → ↑ lipoxygenase) TX: RA, Chronic Inflammation |
|
|
Term
|
Definition
| RA (COX2 Selective) OTH: 1) Least potent of COX-2 inhibitors 2) Does not affect platelet aggregation SE: Can interfere w/antihypertensive therapy Still contraindicated in pts w/GI ulcers TX: RA, Chronic Inflammation |
|
|
Term
|
Definition
| RA (DMARD) MOA: Inhibits DHFR → ↓ thymidylate, ↓ purines, ↓ methionine, ↓ serine SE: Bone marrow (immunosupp) GI Nephro & Hepatotoxicity OTH: Develops resistance via DHFR transport, MPs, Leucovorin (folate) to reverse toxicity TX: RA, CURES: osteosarcoma & choriocarcinoma ALL, Burkitt's, Non-H, Blad |
|
|
Term
|
Definition
| RA (DMARD) MOA: Converted to thioinosinate; Cytotoxic to B/T lymphocytes; Competitive inhibition of inosinate S phase inhibitor MET: Low dose used for prophylaxis SE: Toxicity may limit chronic use OTH: Myelosuppression Coadministration w/allopurinol is toxic (azatioprine broken down by xanthine oxidase) TX: RA, Crohn's, Ulcerative Colitis, Transplant Rejection |
|
|
Term
|
Definition
| RA (DMARD) MOA: Bacteria split azo bond → 5-ASA (& sulfapyridine) → ↓ inflammation MET: 75% reaches colon 5-ASA = active metabolite Sulfapyridine = SEs SE: Nausea, vomiting Headache Allergy OTH: Can cause ↓ folate absorption TX: RA, Ulcerative colitis (85%) Colonic Crohn's Dz |
|
|
Term
|
Definition
| RA (DMARD) MOA: recombinant antibody against TNF-α receptor Admin: SubQ, usually w/ methotrexate SE: Headache, nausea, rash at injection site |
|
|
Term
|
Definition
| RA (DMARD) MOA: binds two molecules of TNF-α together, prevents them from activating cellular receptors Admin: SubQ, combination of methotrexate and etanercept has shown to reduce symptoms in RA more effectively than either one alone SE: Injection site reactions TX: RA |
|
|
Term
|
Definition
| RA (DMARD) MOA: IgG monoclonal antibody directed to TNF-α, inactivating it Admin: IV, used in conjuction w/ methotrexate SE: infusion rxns, fever/chills, anti-infliximab Ab's, predisposition to cell-mediated immunity infections (or reactivations) TX: RA, Crohn's |
|
|
Term
|
Definition
| Tuberculosis MOA: inhibits InhA and KasA, enzymes essential for the synthesis of mycolic acids Admin: oral, PE; absorp. impaired if taken with aluminum-containing antacids MET: met in liver by N-acetylation; rate varies among humans 1-3hrs; INHIBITS CP450 (↑ [phenytoin, benzos, warfarin]) RES: mutation/deletion of katG gene, underproduction of enzyme needed for activation, mut in InhA enzyme = resistance SE: Peripheral neuritis (hands/feet; due to inactivating pyridoxine) Hepatogoxicity jaundice hepatitis (LFT's must be monitored) Rash CNS CROSSES PLACENTA TX: TB, alone as prophylaxis in skin test converters |
|
|
Term
|
Definition
Tuberculosis
MOA: inhibits mycobacterial DNA dep RNA polymerase
MET: Very lipid soluable (penetrates CNS), INDUCES CYP450 (↓ [ketoconazole, warfarin...])
RES: decreased permeability or mutation in DNA dep RNA poly
SE: Red-orange color to secretions Rash Fever GI Flu-like syndrome
TX: TB, prophylaxis against MAC, Leprosy, L. pneumophilia |
|
|
Term
|
Definition
TB
MOA: mycobacterial fatty acid synthase I gene, stops mycolic acid synthesis
MET: oral, high lipophilicity (CNS pen), works best at ↓pH ~within phagolysosomes)
SE: Hepatotoxicity, Gout (inhibits uric acid secretion), Arthralgia and myalgia
TX: short-course (<6 mo) TB in combo w/ isoniazid/rifampin |
|
|
Term
|
Definition
TB
MOA: inhibits arabinosyl transferase, ↓ syn of arabinogalactan, carbohydrate polymer essential in mycobacterial cell wall
Admin: oral, high lipophilicity (CNS pen)
SE: Optic Neuritis, Red-Green color blindness, Gout (↓ uric acid secretion) Rash Fever
TX: M. tuberculosis, M. avium, M. kansasii |
|
|
Term
|
Definition
TB
MOA: binds 30s ribosomal subunit, inhibits formation of initiation complex and blocks translocation step. also induce misreading of mRNA code; transported in via an OXYGEN DEPENDENT system (inactive against anaerobes)
Admin: IV, poor oral absorp (no CNS pen)
RES: modifying enzymes (most common)
SE: amiNOglycoside; Nephrotoxicity (acute tubular necrosis) Ototoxicity (↑ w/ loop diuretics) |
|
|
Term
|
Definition
TB
MOA: 2nd Line TB agent, always given in combo |
|
|
Term
|
Definition
MOA: binds the 50s ribosomal subunit, inhibits translocation step of protein syn
Admin: oral, IV
MET: INHIBITS CYP450
RES: Bacterial plasmids coding for enzymes that inactive the drug
SE: GI Cholestatic hepatitis Hypersensitivity; contraindicated with Theophylline
TX: Alt. to penicillin; Mycoplasma, Legionella, C. trachomatis, C. diphtheriae, B. pertussis |
|
|
Term
|
Definition
Leprosy
MOA: PABA analog that binds DHP
synthetase → ↓ folic acid
Administer: oral or IV
MET: acylation in the liver
RES: Target site mutation, up-regulation,
new genes, altered uptake/efflux
(Plasmid/Chromosomal)
SE:
Allergy
Not given to: G6P or folic acid
deficiency, or pregnant; Drug-induced lupus erythematosus
HIV: prophylaxis → neutropenia &
exfoliative dermatitis
TX: Leprosy in combo w/ rifampin and clofazimine |
|
|
Term
|
Definition
Leprosy
MOA: binds DNA and inhibits its replication
Admin: oral
SE: Distinctive reddish-brown discoloration of the skin, GI
TX: Leprosy |
|
|
Term
|
Definition
| Gout MOA: Comp. inhibits xanthine oxidase ↓conversion of hypoxanthine → xanthine → uric acid MET: Metabolized to oxipurinol (active) Depletes purine precursors (5'-PRPP) SE: Maculopapular rash (pruritus) GI, hepatotoxicity Fever, hypersensitivity OTH: Not useful for acute gout attacks Inhibits kidney reperfusion injury TX: Chronic tophaceus gout |
|
|
Term
|
Definition
| Gout (exact same as allo) MOA: Comp. inhibits xanthine oxidase ↓conversion of hypoxanthine → xanthine → uric acid MET: Metabolized to oxipurinol (active) Depletes purine precursors (5'-PRPP) SE: Maculopapular rash (pruritus) GI, hepatotoxicity Fever, hypersensitivity OTH: Not useful for acute gout attacks Inhibits kidney reperfusion injury TX: Chronic tophaceus gout |
|
|
Term
|
Definition
| Gout MOA: Inhibits proximal tubule reabsorption of urate MET: Admin: oral Half-life: 6-12 hours Interax: PCN, ASA, sulfa, allopurinol SE: GI Dermatitis Nephrotic syndrome OTH: Not to be used in acute gout attacks TX: Hyperuricemia control |
|
|
Term
|
Definition
| Gout MOA: Binds microtubule tubulin → ↓polymerization → ↓WBC migration & urate phagocytosis MET: Admin: oral Accumulates in WBCs Deacetylated in liver SE: GI Blood dyscrasias CNS depression, shock TX: 2nd line acute Gouty arthritis attacks Pseudogout Familial Med. fever |
|
|
Term
|
Definition
| Gout MOA: recombinant enzyme which catalyzes uric acid → allantoin which is 5x-10x more soluable than uric acid i.e. More effective renal clearance of uric acid SE: Methmegloginemia Anaphylaxis Expense OTH: catalyzes conversion of existing uric acid TX: Gout |
|
|
Term
|
Definition
| Anti-fungal MOA: polyene; binds to ergosterol and forms pores w/in memb Admin: IV, intra-thecal (fungal meningitis), topial (candidiasis) MET: poor absorption from GI, excreted in bile RES: replace ergosterol with other precursor sterols SE: Renal Impairment (80% experience ↓ GFR and changes in tubular function) Renal Tubular Necrosis Hypotension Fever chills Hypochromic normocytic anemia CNS TX: Systemic mycosis (Candida, Histoplasma, Cryptococcus, Aspergillus, Coccidioides, Mucor) |
|
|
Term
|
Definition
| Anti-fungal MOA: inhibits DNA synthesis by conversion to 5-fluorouracil (thymidalate synthase inh) Admin: PO, distributes well (inc CNS) SE: Hematological (reversible bone marrow depression) Elevatd hepatic enzymes GI TX: adjunct to systemic infections (Candida, Cryptococcus) |
|
|
Term
|
Definition
| Anti-fungal MOA: blocks cytochrome p-450-mediated Ergosterol synthesis (c-14-α demethylase) Admin: PO MET: depends on gastric acidity to be dissolved and absorbed; Cimetidine and antacids impair its absorption; met in liver excreted in bile SE: Gynecomastia (inhibits sterol synthesis), dec libido, GI, Hepatic dysfunction, INHIBITS CYP450, Allergies OTH: never use azoles and ampho B together, antagonistic TX: Blastomyces, Coccidioides, Histoplasma, Candida albicans; hypercortisolism |
|
|
Term
|
Definition
| Anti-fungal MOA: blocks cytochrome p-450-mediated Ergosterol synthesis (c-14-α demethylase) Admin: IV, oral MET: INHIBITOR of CYP450, does not cross the BBB SE: GI, hypertriglyceridemia, rash, hypokalemia, hypertension, Hepatotoxicity (does not have endocrinological SE of Keto) TX: indolent nonmeningeal infections of blastomycosis, histoplasmosis, coccidioidomycosis and cutaneous sporotrichosis |
|
|
Term
|
Definition
| Anti-fungal (echinocandins) MOA: inhibits cell wall synthesis by blocking the formation of β(1,3)-D-glucan Admin: IV SE: Phlebitis at injection site TX: Invasive Aspergillus for pts who have failed therapy with other agents (ampho b, voriconazole) |
|
|
Term
|
Definition
| Anti-Fungal (s7s drugs for mucocutaneous) MOA: inhibits microtubule function, with long-term therapy, this drug accumulates in the newly synthesized stratum corneum MET: well abs orally, esp with high fat diet; elim bile SE: Headache, Hepatotoxicity, GI, rarely teratogenic/carcinogenic TX: Dermatophytes (Trichophyton, Microsporum, Epidermophyton) |
|
|
Term
|
Definition
| Anti-Fungal (sys Rx for mucocutaneous) MOA: inhibits squalene epoxidase which syn ergosterol, accum of squalene is toxic to fungi Admin: oral or topical SE: Rash Headache GI, contraindicated in pregnancy TX: first-line Dermatophyte infections, esp onychomycosis |
|
|
Term
|
Definition
| Anti-Fungal MOA: inhibits production of Ergosterol Admin: orally or IV; elim through kid MET: enters the CSF in high concentrations and is not dep on acidic pH for abs. does not cause endocrine dysfunction (keto) SE: GI Headache Rash, INHIBITS CYP450 (↑ [cyclosporine, warfarin, phenytoin]), Teratogenic TX: DOC Disseminated or progressive coccidioidal infections, Disseminated histoplasmosis, Oral, esophageal, and vaginal candidiasis, Prophylaxis of cryptococcal meningitis in AIDS pt |
|
|
Term
|
Definition
| Anti-Fungal MOA: inhibits ergosterol synthesis Admin: oral, IV MET: met. by CYP450, influenced by other drugs effects on cyp450 SE: blurred vision or color perception, Hepatotoxicity, Rash TX: invasive Aspergillosis, life-threatning infections with Fusarium or Scedosporium apiospermum |
|
|
Term
|
Definition
| Anti-Fungal (topical) MOA: polyene sim. to ampho B, creates pores in cell membrane by binding to Ergosterol SE: Bitter taste, nausea TX: topical for skin & mucocutaneous inf. or Oral for Candida thrush. "swish and swallow" |
|
|
Term
|
Definition
| Anti-fungal (topical) MOA: inhibits c-14-α demethylase, blocks Ergosterol synthesase SE: itching, erythema, burning TX: Superficial infections of th skin and mucous membranes (Blastomyces, Coccidioides, Histoplasma, Candida albicans) Effective against Candida and dermatophytoses |
|
|
Term
|
Definition
| Anti-fungal (topical) MOA: inhibits c-14-α demethylase, blocks Ergosterol synthesase SE: itching, erythema, burning TX: Superficial infections of th skin and mucous membranes (Blastomyces, Coccidioides, Histoplasma, Candida albicans) Effective against Candida and dermatophytoses |
|
|
Term
|
Definition
| Anti-fungal (topical) MOA: inhibits squalene epoxidase blocking Ergosterol synthesis Admin/TX: creams for tinea cruris and corporis |
|
|
