- blocks voltage gated Na channels

- selective for fast acting neurons (Na channels in unactivated state)

 - anti-epileptic drug,  neuropathic pain , trigeminal neuralgia

- blocks alpha 2 delta subunit of Ca ion channels in presynaptic neuron .blocking NT release of glutamate, substance P -

Used for : seizures, neuropathic pain

Blocks thiolase.. long term use in chronic angina pectoris if other drugs dont work

Inhibits B-oxidation--> enhances glucose oxidation and maintains a high level of ATP  

GABA-a receptor modulator (narrow range of subtypes)

Use: when chief complaint is insomia

GABA-B receptor agonist

Use: in muscular spasm movements

D2- receptor competitive antagonist

- given in schizophrenia (last resort)

a2 adrenoceptor agonist

- ADHD, neuropathic pain

D2 agonist

D2>>D1

D2 agonist = decrease prolactin secretion (antagonist would increase prolactin secretion)

Use: hyperprolactinemia (prolactin secreting adenomas)

High doses reduces GH circulation

Adverse: nausea, vomiting (due to area postrema), divided doses avoid this 

- 2 amino acid difference from vasopressin

- IV or intranasally (less critical patients)

- uterine contractions (induction of labor, postpartum)

- milk letdown

(ADH)

V1- contract arterial ss

V2- basolateral cells of distal and collecting duct= antidiuretic effect. (extrarenal= ^ VIII, von willebrand factor)

Use: ER situation for V1 (cardiac life support, esophageal varicosities)

D-Arg instead of L-Arg( long t=1/2..)

analog of vasopressin, V2

orally (<1%), nasal (3-4%, central DI), IV

Use: diabetes insipidus, von willebran disease type 1, hemophillia A, nocturnal enuresis

Adverse: hyponatremia

GHRH

diagnostics

Somatostatin analog

45X more potent than somatostatin and (t1/2=80 mins)

subcutanous 3x/day and IM (1/mo)

Use: acromegaly, tumors

Adverse: GI problems, vit B12 deficiency

recombinant GH

subcutaneous

Use: pituitary dwarfism

Adverse in children: scoliosis (growth to rapid), diabetes mellitus (due to increase in insensitivity), headache

Adverse in adults: diabetes mellitus, carpal tunnel, arthritis (same symptoms seen in acromegly)

GH antagonist

Use: acromegaly if octreotide is not working

r-IGF-1

Use: laron dwarfism if there is a lack of response to GH (antibodies for GH, mutated receptor)

Give with IGFBP-3 (main carrier, ^t1/2)

give with snack (b/c hypoglycemia side-effect)

T4

oral, IV (myxedema coma T3,T4)

treatment of choice

long 1/2, circulates bound to TBG, depot

Dose adjustment if change in [TBG]

131: destruction of thyroid (could become hypo give levo, T4)

123: gamma rays only, imaging

thyroid storm- 14 days

decreases vascularity, size

inhibits thyroid peroxidase

slow onset

prefered in pregnancy

Adverse: Agranulocytosis

high doses of  propylthiouracil

Corticosteriods

Propranolol- also helps with hyperthyroid symptoms like: tachycardia, tremor, sweating

PGE1

Intraurethral, IV, intracavernous

MOA: relaxation of ss, vasodilation, inhibits platelet aggregation

Use: patency of ductus arterioses, penile erection

WARNING: potential apnea in neonates

Contra: Not given to people with sickle cell anemia, deformities

PGF2-alpha

eye drops

prodrug (esterases in cornea)

25% excretion in feces

MOA: increases outflow of aqueous humor from anterior chamber, ^ eyelashes

Use: eyelash hypotrichosis, ocular hypertension, open angle glaucoma

PGF2-alpha

IM

MOA: stimulates uterine contraction (which halts bleeding)

USE: induction of 2nd trimester abortion, refractory postpartum uterine bleeding

PGE2

vaginal gel/dipository

MOA: induction of uterine contractions, cervical ripening (^cervical collagenase activity), relaxes cervical smooth muscle, ^ sensitivity to oxytocin

Use: gel --ripening of cervix, suppository---abortion 2nd trimester

PGF2-alpha

eye drops, prodrug

MOA: ^ outflow of aqueous humor from anterior chamber

Use: open angle glaucoma, ocular hypertension

Changes pigmentation of IRIS to BROWN

PGF2-alpha, prodrug

MOA: lowers intraocular pressure by ^^ outflow of aqueous humor from the anterior chamber

Use: open angle glaucoma, ocular hypertension

PGf-2a

eye drops, prodrug

MOA: lowers intraocular pressure by ^ outflow of aqueous humor from anterior chamber

Use: open angle and ocular hypertension  (if nonresponsive to others)

Use: replacement therapy to treat/prevent osteomalacia and rickets

during renal failure

low calcitriol--> low Ca G.I absorption--> hypocalcemia--> hyperparathyroidism, ^ bone resorption

Adverse: hypercalcemia, b/c bypass feedback mechanism

Ca-sensing receptor activator

allosteric modulation of the Ca receptor potentiates the response to Ca--> decreases PTH

Use: primary hyperparathyroid, secondary hyperparathyroid ( renal failure), parathyroid carcinoma

Adverse: hypocalcemia, cardiac effects  

parathyroid hormone analog

Use: promote bone formation, if given as burst only, in severe osteoporosis. Wont work if PTH is chronically elevated.

Helps move Ca in bone

Excretes Ca in kidney

Direct inhibition of osteoclast-- great in ^ bone turnover disease

analgesic effect

selective agonist of PPARy making the cell more responsive to insulin

primarly targets fat

MOA: activation AMPK

decreases hepatic gluconeogenesis, glycogenolysis

inactivates ATP-K channel

^K--> depolarization--> ^ intracellular Ca --> insulin release

GLP-1 receptor agonist

supresses glucagon secretion, decreases appetite, ^ insulin release

Hydrocortisone = glucocorticoid (600x more than mineral)

Fludrocortisone = mineralocorticoid

treat in addison's disease-- oral

Addisonian crisis = IV hydrocortisone

glucocorticoid (anti-inflamm):

Dexamethasone> fludrocortisone>Prednisone> hydrocortisone

Mineralcorticoid ( Na retaining):

Fludrocortisone > Hydrocortisone> prednisone

inhibits P450 enzymes--> no steroid biosynthesis

UseL cushings disease/syndrome

Adverse: gynecomastia (androgen synthesis inhibited)

glucocorticoid receptor antagonist

Use: cushings syndrome (tumors)

Aluminum Hydroxide/Magnesium Hydroxide

aka Maalox

Antiacids

Magnesium---diarrhea

Aluminum--- constipation

Antiacid

Produces CO2

USe: Hypocalcemia, Hyperphosphatemia, Osteoporosis prevention

Adverse: flatulence, milk-alkali syndrome, hypercalcemia, hypophosphatemia

Sodium Bicarbonate/aspirin/citric acid

aka

Alka-Seltzer

Antiacid, inhibit cox-1, cox-2

USE: heartburn, upset stomach

MOA: H2-Receptor antagonist--> decrease [cAMP] in parietal cells

This drug inhibits  CYP enzymes in liver-other drugs wont be broken down

USE: PUD,GERD

Adverse: long term leads to gynecomastia, galactorrhea b/c it  blocks dihydrotestosterone binding to androgen receptor--> estradiol can be broken down, ^[prolactin]

MOA: H2-Receptor antagonist--> decrease [cAMP] in parietal cells

USE: PUD, GERD

MOA: H2-Receptor antagonist--> decrease [cAMP] in parietal cells

USE: GERD, PUD

MOA: irreversible inhibition of H/K ATPase, pro-drug

Taken on empty stomach

Pharmkinetics: Ideal, short t1/2, conc. and activated at site of action, long duration

Serum Gastrin levels will be 2x higher

USE: GERD,PUD Most effective drug for treatment of H. Pylori (with clarithromycin, Amoxicillin) 14days but PPI for 6 weeks  

Adverse: chronic use: hip,wrist, spine fracture, resp infections, polyps, inflammation

MOA: irreversible inhibition of H/K ATPase, pro-drug

Taken on empty stomach

Pharmkinetics: Ideal, short t1/2, conc. and activated at site of action, long duration

Serum Gastrin levels will be 2x higher

USE: GERD,PUD Most effective drug for treatment of H. Pylori (with clarithromycin, Amoxicillin) 14days but PPI for 6 weeks  

Adverse: chronic use: hip,wrist, spine fracture, resp infections, polyps, inflammation

sucrose complexed with aluminum-OH

Band- aid over ulcer and erosions

Adverse: constipation and Bezoar formation

Analog of PGE1

oral, vaginal, rectal

Pharma actions: stimulates mucus, electrolyte and fluid in GI. ^ mucosal blood flow, ^uterine contractions , ^ intestinal motility.

USES:  NSAID induced ulcers, PUD, early abortion,  induce labor, post partum hemorrhage

Adverse: Diarrhea, abdominal pain

D2 antagonist

antiemetic and gastroprokinetic agent

Adverse: gynecomastia, galactorrhea

Macrolide antibiotic

IV

MOA: stimulation of motilin receptors--> MCC

USEs: gastroparesis but develops tolerance---reason its only used in procedures and not neuropathies , promotes gastric emptying of blood beofre endoscopy

hog pancreas

oral with food

time released because need to bypass low pH of stomach so that enzymes wont be destroyed

Bismuth subsalicylate

(Pepto-Bismol)

coats the GI

salicylate: antisecretory effect

Bismuth: antimicrobial effects

USES: dyspepsia, heartburn

Adverse: Reye syndrome, salicylate toxicity

oral

wide distribution

prodrug--> 1st pass--> albendazole sulfoxide

MOA: inhibit helminthic microtubule synthesis, larvae and ovicidal

Use: tropics einosiophilia,  Ascariasis, Cutaneous larva migrans,  A. cantonensis,  Gnathostomiasis, hookworm (americanus, duodenale),  Hydatid disease, intestinal capillariasis, Loiasis, Neurocysticercosis,  visceral larva migrans

oral

wide distribution

MOA: inhibit helminthic microtubule synthesis, blocks glucose uptake on larvae and ovacidal

Use: drug of choice:

Enterobiasis

Trichinosis

Trichuriasis

A. Cantonensis

Ascariasis

Hookworm

T. Orientalis

Need to apply for the drug from CDC

Use: Filariasis, loiasis, tropical eosinophila, Mansonella streptocerca  (adults die slower, dosage is longer)  intial low dosage

MOA: binds to glutamate gated channels--> ^ Cl

oral-- scabies

topical--lies

Use: Onchocerca volvulus (river blindness, up to 10 yrs)

Strongyloidiasis

Cutaneous larva migrans

MOA: increase permeability to Ca

Use: Diphyllobothrium latum, Hymenlepis nana, Fasciolopsis buski, Heterophyes Heterophyes, Metagonimus yokogawai, Schistosomiosis, Clonorchiasis, opisthorchiasis, Paragonimiasis, Taeniasis

Not to use in OCULAR or SPINAL cysticercosis b/c its very  effective --> ^ inflamm

MOA: stimulates release of ACh, inhibits action of cholinesterase---> muscle paralysis

Use:  

Ascariasis

Enterobiasis

Hookworm disease

Trichostrongylus orientalis

Tetracycline antibiotic

MOA: kills Wolbachia an intracellular bac symbiont of filarial parasites in W. bancrofti and onchocerciasis

Antiprotozoal agent

dracunculiasis

Antiprotozoal agent

alternative to H. nana

MOA: Inhibits ADH receptors at medullary collecting duct

Conivaptan= V1 too     Tolvaptan = V2 only

USE: SIADH, chronic euvolemic Hyponatremia (b/c diuresis effects water more than Na)

Other organs: Inhibitors of CYP3A4

aldosterone receptor antagonist, potassium sparing , late distal convoluted tubule and collecting

slow onset , antiandrogen

MOA: Reversible inhibits carbonic anhydrase in proximal tubule (cytoplasm, brush border)

Use: Open angle, edema, acute mountain sickness (^ [H] plasma--> ^ ventilation), Epilepsy (^[Na]tissue--> hyperpolarization), Alkalosis due to loop diuretics 

Renal effects:

   - ^ excretion: Na,HCO3, K ( b/c  the NCCK in TAL and ENac in collecting increase activity)

- Decrease excretion of H, NH4-- both powered by Na

- Metabolic acidosis + hyperchloremia

- complete tolerance due to acidosis, low efficacy

Other organs: Inhibition of CA in ciliary body, choroid plexus

Adverse:  hypokalemia, nephrolithiasis (Ca +alkaline urine), sulfa type allergy

MOA: Reversible inhibits carbonic anhydrase in proximal tubule (cytoplasm, brush border)

Use: Open angle, edema, acute mountain sickness (^ [H] plasma--> ^ ventilation), Epilepsy (^[Na]tissue--> hyperpolarization), Alkalosis due to loop diuretics 

Renal effects:

   - ^ excretion: Na,HCO3, K ( b/c  the NCCK in TAL and ENac in collecting increase activity)

- Decrease excretion of H, NH4-- both powered by Na

- Metabolic acidosis + hyperchloremia

- complete tolerance due to acidosis, low efficacy

Other organs: Inhibition of CA in ciliary body, choroid plexus

Adverse:  hypokalemia, nephrolithiasis (Ca +alkaline urine), sulfa type allergy

MOA: osmotic diuretic (mainly at thin desceding loop, some at proximal tubule)

Use: Cerebral edema, acute angle closure

Renal effects:

 - low solvent drag, increase secretion of everything

 - good efficacy

Other organs: water is pulled from IC--> EC--> blood  this reduces intracranial, intraocular pressure

Adverse: Drug leaves body too quick, ^GFR = hypovolemia vs Drug doesn't leave body, EC volume expansion= hypervolemia, hyponatremia, pulmonary edema

Contra: low GFR, heart failure, pulmonary congestion, dehydrated patients

sulfonamide loop diuretic-- inhibits NCCK. BEST

Uses: Pulmonary, renal edemas, Ascites, Hypertension, hypercalcemia

Renal effects:

 - no (+) lumen= decrease in Ca, Mg reabsorption

 -  medulla not hypertonized well

 - Macula densa insensitivity--> potential ^ GFR sense Macula densa doesnt sense NaCl

 - small inhibition effect on CA

Adverse: Hypokalemic metabolic alkalosis, hypo-Mg,volemia,

 loop diuretic-- inhibits NCCK. BEST

Uses: Pulmonary, renal edemas, Ascites, Hypertension, hypercalcemia

Renal effects:

 - no (+) lumen= decrease in Ca, Mg reabsorption

 -  medulla not hypertonized well

 - Macula densa insensitivity--> potential ^ GFR sense Macula densa doesnt sense NaCl

 - small inhibition effect on CA

Adverse: Hypokalemic metabolic alkalosis, hypo-Mg,volemia,

Thiazide----Moderate

MOA: inhibits NaCl symporter in early distal convoluted tubule and weak inhibitor of CA

Use: Hypertension 1st line, Edema,  Nephrogenic diabetes insipidus (hypovolemia induced ^ NaCl and water reabsorption at proximal tubule= low water delivery to ADH areas)

Renal effects: Decreased excretion of Ca, NH4, metabolic alkalosis

Moderate

MOA: inhibits NaCl symporter in early distal convoluted tubule and weak inhibitor of CA

Use: Hypertension 1st line, Edema,  Nephrogenic diabetes insipidus (hypovolemia induced ^ NaCl and water reabsorption at proximal tubule= low water delivery to ADH areas)

Renal effects: Decreased excretion of Ca, NH4, metabolic alkalosis

Triamterene/amiloride

MOA: Androgen receptor antagonist

USE: Dont give by itself, why?

Pharmakinetics:  oral (not a steriod)

MOA: 5-alpha reductase inhibitor

USE: male pattern baldness, female hirsuitism

1. given as IM especially in children

2.  can be given orally  but hepatotoxic

MOA: GnRH agonist

USE: chronic exposure shuts down axis

PK: IM depot