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Pharm Opioids, etc...
Crazy
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Medical
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12/18/2012

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Term
Morphine
Definition
Stimulates all opioid receptors, used in severe pain; more effective IV; short half life; duration 4-6 hours; metabolized by CYP2D6
Term
Hydromorphone (Dilaudid)
Definition
Strong analgesic that acts on all opioid receptors; effective for severe pain; more potent than morphine
Term
Methadone
Definition
Stimulates mu receptors; long half-life; Maintenance tx of addicts
Term
Meperidine (Demerol)
Definition
Mu agonist that causes euphoria; short-acting drug; metabolites cause seizures, so can't use in high doses or for long term; NO cough suppression; anticholinergic; less constipation, urinary retention; serotonin syndrome with MAOIs
Term
Fentanyl
Definition
Opioid that is lipid soluble and highly potent; short duration of action and half-life; HIGH abuse potential; used in short surgical procedures; can cause truncal rigidity if given rapidly IV; transdermal patches or lollipops; metabolized by CYP
Term
Heroin
Definition
Opioid Schedule 1 drug; very potent and gets into brain well; commonly abused; prodrug for morphine
Term
Hydrocodone
Definition
Opioid prodrug used for moderate to severe pain; combined with acetaminophen; short half-life
Term
Oxycodone (OxyContin)
Definition
Opioid used for moderate to severe pain; used also for Tourette's and restless leg syndrome; metabolized by CYP
Term
Codeine
Definition
Opioid used for moderate pain; also a cough suppressant; metabolized by CYP
Term
Pentazocine
Definition
Kappa receptor agonist; Mu receptor partial agonist; used for moderate pain; less sedating than other opioids; may cause dysphoria; low abuse potential
Term
Buprenorphine
Definition
Partial agonist on mu receptors; ceiling effect, not much euphoria; absorbed from buccal mucosa; combined with naloxone, injected won't work
Term
Percoset
Definition
Oxycodone combined with acetaminophen
Term
Tramadol
Definition
Weak mu agonist; inhibits NE/5-TH reuptake; causes seizures when combined with antidepressants, serotonin syndrome; low abuse potential
Term
Tapentadol
Definition
Mu receptor agonist, inhibits NE reuptake, stimulates a2 receptors; used for moderate to severe pain; also for neuropathic pain; schedule II
Term
Dextromethorphan
Definition
NO effect on mu receptors; only cough suppressant; Blocks NMDA receptors, which means abuse potential; decreases 5-HT uptake; cough syrup abuse in teenages, causes death
Term
Naloxone (Narcan)
Definition
Opioid antagonist that is only injected; short acting
Term
Percodan
Definition
Oxycodone combined with aspirin
Term
Naltrexone
Definition
Opioid antagonist that is long-acting; will precipitate withdrawal; has liver toxicity; treatment of opioid addicts
Term
Methylnaltrexone, Alvimopan
Definition
Opioid antagonists that are peripherally acting used for treatment of opioid induced constipation; DO NOT reverse centrally-mediated analgesia, respiratory depression; one is IV, the second oral
Term
Nitrous oxide
Definition
Analgesic gas not very soluble in the blood with a rapid induction; very potent and used in most anesthesia mixtures to speed induction; does not cause malignant hyperthermia; causes euphoria, relaxation, warmth
Term
Halothane
Definition
Potent slow induction inhaled anesthetic; not used very much any more; causes ventilatory depression and bronchodilates; inhibits gag reflex and cough reflex; sensitizes the heart to catecholamines, causes arrhythmias; can cause HEPATITIS; can cause malignant hyperthermia, tx with ?
Term
Enflurane
Definition
Anesthetic gas that is faster than halothane; no heart changes, but can cause seizures; metabolism can cause fluoride and renal toxicity; not used very much
Term
Isoflurane
Definition
Potent inhaled anesthetic; very non-toxic; rapid induction and recovery, but bad taste so used only for perpetuation; decreases BP and increases HR; used in neurosurgery; potentiates neuromuscular blocking agents
Term
Sevoflurane
Definition
Inhaled anesthetic that has rapid induction and recovery; low airway irritation and low toxicity; used in children; safest in CV disease
Term
Desflurane
Definition
Very fast induction inhaled anesthetic; irritating to airway, don't use for induction; decreases BP and increases HR; causes respiratory depression and increases ICP; low toxicity
Term
Thiopental
Definition
Short acting barbituate used in induction of anesthesia; CI for porphyria; little analgesia; severe respiratory depression
Term
Propofol
Definition
The perfect anesthetic; may facilitate GABA; fast acting and quick recovery IV, used for maintenance of anesthesia, can be used for short or long surgeries; causes some respiratory depression (don't necessarily have to ventilate the patient); anaphylaxis biggest side effect due to albumin in emulsion; lidocaine added to decrease pain on injection site
Term
Etomidate
Definition
Fast acting IV anesthetic used for fast onset of action and short duration; causes hiccups, hypotension; can exacerbate seizures
Term
Ketamine
Definition
Causes dissociative anesthesia and potent analgesic; binds to PCP site on NMDA receptor; increases HR and BP; causes emergence delirium in adults, tx with benzos; little N/V; used in vet med and children; drug of abuse (teens like drugs that act on NMDA receptors)
Term
Amphetamines (abuse)
Definition
Increases release of DA; used to treat narcolepsy, ADHD; causes alertness, euphoria, excitement, appetite suppression; aggression, paranoia, delusions; increases BP
Withdrawal is fatigue, increased appetite
Term
Methamphetamine (abuse)
Definition
Increases release of DA and NE in basal ganglia; may produce amphetamine psychosis
Chronic use may cause neurotoxic damage, personality changes
Intense craving, severe withdrawal
Cardiac toxicity; weight loss, whiter skin, dental problems, seizures, stroke, organ damage, lack hygiene, bugs cause them to scratch and have open sores
Term
Cocaine
Definition
CNS stimulant that inhibits DA and NE reuptake; ingredient in Coca-cola until 1903; CNS stimulation to cause alertness, euphoria, anxiety, hyperactivity; severe craving
Can be used medically as a local anesthetic, vasoconstrictor
Causes tachycardia, vasoconstriction, HTN, bronchodilation, increased body temp, dilated pupils
Crack kind inhaled rapidly absorbed, very fast onset; crack babies retarded growth, stillbirths
Chronic use causes reduction in overall brain activity; anxiety, insomnia, paranoia, hallucinations
Bugs they try to get out
Overdose causes Vtach, fibrillation; stroke, seizures
Bromocriptine decreases craving
Term
Nicotine
Definition
Activates nicotinic receptors in CNS and periphery; increases 5-HT and DA release; CNS increased arousal, appetite suppression
Short half life
Very reinforcing and highly addictive
Bupropion used to decrease craving
Term
MDMA, Ecstasy
Definition
Increases 5-HT activity by blocking reuptake and stimulating 5-HT receptors
Produces feelings of peacefulness, empathy, closeness, trust; may be followed by confusion, depression, anxiety, paranoia
Increases BP, HR; causes hyperthermia, dehydration, kidney failure
Persistent memory loss may occur
Decreased cerebral blood flow
Term
Marijuana (THC)
Definition
Binds to presynaptic cannabinoid receptors; inhibits release of glutamate and ACh
Quickly absorbed, lipophilic, which means stored in fat and long half life
Mild euphoria, well being, altered sense of time, tranquility
NO physical dependence; psychological dependence possible
Decreased memory over time, amotivational syndrome, decreased testosterone and sperm production in males
LBW, fetal malformations
Medical uses: bronchodilation, antiemetic, appetite stimulation (Dronabinol), analgesia, decreased spasticity/ataxia/muscle weakness, decreased intraocular pressure
Bath Salts synthetic cannabinoid receptor agonists; psychoactive effects
Term
LDS, mescaline (mushrooms), psilocybin (peyote)
Definition
Acts on 5-HT receptors in brain
Euphoria, visual hallucinations that last hours
Bad trips and flashbacks
Synesthesia--one sensory modality assumes characteristics of another
NO dependence because they don't stimulate DA pathways
Term
PCP, Ketamine, GHB
Definition
NMDA receptor antagonists used as general dissociative anesthetics
Sensation of dissociation or floating
Can produce psychosis, treat with haloperidol
Analgesia accompanied by aggression, dangerous combination
Increases BP
Term
Cocaine
Definition
Ester-type local anesthetic; short-acting, used around URT; inhibits Na channels, and secondarily can increase DA and NE in the CNS; Schedule II
Term
Benzocaine
Definition
Ester-type local anesthetic; very lipophilic and pKa of 3.5, always in non-ionized form
Used topically only to treat sunburn, minor burns, pruritis
Risk of methemoglobinemia
Term
Procaine
Definition
First synthetic local anesthetic; ester-type; metabolized by pseudocholinesterases
Short duration of action
Metabolic product PABA inhibits sulfa drugs
Used for infiltration anesthesia and diagnostic nerve blocks
Minimal toxicity
Term
Tetracaine
Definition
Ester-type local anesthetic; slow onset of action; 10X stronger than procaine; causes severe toxicity in peripheral blocks
Used in spinal and ophthalmological procedures
Term
Lidocaine
Definition
First amide-type local anesthetic; metabolized in liver by CYP
Wide range of uses; perferred for infiltration blocks and epidural anesthesia
Rapid onset
Risk of TNS in spinal blocks
Greater potency and duration than procaine
Term
Bupivacaine
Definition
Amide-type local anesthetic; long duration of action; used for spinal and epidural anesthesia, infiltration blocks
Greater cardiotoxicity than other amides
More potent sensory than motor block, so better for labor in pregnancy
Term
Ropivacaine
Definition
Amide-type local anesthetic; long-acting; enantiomer of bupivicaine
Less lipid soluble, cleared more rapidly than bupivicane
Metabolized by CYP
Used for peripheral and epidural blocks
Vasoconstricts at clinical doses
Term
Prilocaine
Definition
Amide-type local anesthetic; intermediate duration of action
Highest rate of clearance of amides
Methemoglobinemia due to metabolites
Give methyl blue to treat
CI in cardiac and respiratory diseases
Limited to dental anesthetic
Term
Mepivicaine
Definition
Amide-type local anesthetic; intermediate duration
Not used in labor or topically, just peripheral
Term
Dibucaine
Definition
Amide-type local anesthetic; NOT used in US
Toxic
"" Number Test: measure of butyrylcholinesterase activity
Term
Etidocaine
Definition
Amide-type local anesthetic; long duration of action
Rarely used
Inverse differential block, motor before sensory block
Term
Dinoprostone (PGE2)
Definition
Prostaglandin drug used for abortions, facilitating labor and treating dysmenorrhea; causes vasodilation, bronchial relaxation, and activates GI; initiates uterine contractions; can cause fever and facilitate bone resorption
Term
Alprostadil (PGE1)
Definition
Prostaglandin drug given by injection for tx of ED; can cause penile pain and priapism; also used in peds to keep ductus arteriosus open before surgery; causes vasodilation by decreasing intracellular Ca, bronchial muscle relaxation, activates GI, relaxes SM in corpus cavernosum, produces fever and facilitates bone resorption
Term
Prostacyclin (Epoprostenol)
Definition
Prostaglandin drug used to relieve primary pulmonary HTN
Term
Latanoprost
Definition
Analog of prostaglandin F2a; increases resorption of aqueous humor; topical, one drop in the evening; can cause blurred vision, conjunctival hyperemia, irritation
Term
Zileuton and Zafirlukast and Montelukast
Definition
LT receptor inhibitors that are used to treat asthma
Term
Misoprostol
Definition
PGE1 analog used to reduce gastric acid secretion in ulcers
Term
Aspirin (acetasalycilic acid)
Definition
Nonselective, irreversible inhibitor of COX-1 and COX-2; causes analgesia, antipyretic, anti-inflammatory by inhibiting synthesis of factors involved in chronic inflammation and platelet effects; analgesia due to peripheral and CNS effects in hypothalamic area, also prevents sensitization of pain receptors to stimuli; lowers body temp only in situations where elevated body temp is due to conditions that raise the hypothalamic thermostat
Fast oral absorption, slowly crosses BBB; rapidly hydrolyzed in plasma; competes with other drugs for plasma protein binding sites
High doses metabolized by zero order kinetics
Alkalinization of urine promotes excretion
Term
Celecoxib
Definition
Selective reversible COX-2 inhibitors; less GI adverse effects and platelet aggregation
Increased risk of CV disease
CI in GI disease, asthma, breast feeding, pregnancy, renal failure
Term
Indomethacin
Definition
Reduces PMNs, inhibits phospholipase A
COX inhibitor
Worst side effects because very potent
Term
Diclofenac
Definition
Potent COX inhibitor; decreased AA bioavailability; mostly GI side effects
Term
Ketorolac
Definition
COX inhibitor that can be used in postsurgical pain; can't be used for more than 5 days or see gastric ulcerations
Term
Ibuprofen (Motrin)
Definition
OTC COX inhibitor; DOC
Term
Naproxen
Definition
COX inhibitor suitable for long term treatment
Longest half life, best for fewer daily doses
Term
Piroxicam
Definition
COX inhibitor NSAID; recognize the name
Term
Nabumetone
Definition
Prodrug COX inhibitor
Long half life
Term
Phenylbutazone
Definition
Very potent NSAID, produces a lot of GI sxs; not marketed
Term
Acetaminophen
Definition
NOT inhibitor of peripheral COX enzyme; unknown mechanism of analgesia; NOT anti-inflammatory or anti-rheumatic
Antipyretic and analgesic only
Overdose causes fatal hepatic necrosis
Hepatotoxicity can progress to encephalopathy and death
Requires only 25 grams
Term
Gold Salts
Definition
Inhibition of phagocytosis; used to treat rheumatoid arthritis; decreases immune functions of macrophages because they eat this drug
Causes bone marrow damage, enterocolitis
Term
Penicillamine
Definition
Used for rheumatoid disease and Wilson's disease; may be as effective as gold
Term
Hydroxychloroquine
Definition
Antihistaminic, anticholinesterase, antiprotease properties; used to treat rheumatoid disease
Term
Sulfasalazine
Definition
Used to treat RA and IBD; better tolerated, equally effective to gold
Term
Infliximab
Definition
Antibody against TNF-a; used for Crohn's and RA; must be given IV
Term
Rituximab
Definition
Antibody that is chimeric; binds to CD20; treats lymphoma and leukemia
Term
Adalimumab
Definition
Antibody against TNF-a; used to treat RA; 100% human peptide sequence
Term
Etanercept
Definition
Fusion protein made by DNA technology; fake TNF-a receptor to inhibit TNF-a activity
Administered subQ
Term
Abatacept
Definition
Fully human fusion protein that competes with CD28 for APC binding; used to treat RA
Term
Leflunomide
Definition
Inhibits dihydroorotate dehydrogenase, used in de novo pyrimadine synthesis; inhibits induction of COX-2
Leukocytes pyrimidine 90% comes from de novo pathway, so inhibits leukocytes, but not other cells (which only use de novo pathway for 10%)
Term
Mycophenylate mofetil
Definition
Inhibits lymphocyte purine synthesis; used to treat RA
Prodrug
GIven orally or IV
Term
Anakinra
Definition
Interleukin-1 receptor antagonist; recombinant
Used to treat RA
Given subQ
Term
Cochicine
Definition
Binds tubulin to inhibit assembly of microtubules; anti-inflammatory by inhibiting migration of PMNs
Used in gout for acute attacks
NO analgesic effect
Effective 12-24 hours
Side effects diarrhea
Term
Probenecid
Definition
Uricosuric agent
Maintain large urine volume to avoid kidney stone formation
Give prophylactic colchicine to avoid initial gouty attack
Decreases excretion of acidic compounds or metabolites
Term
Allopurinol, Feboxostat
Definition
Inhibit xanthine oxidase
Effective in primary and secondary gout
Serious vasculitis, agranulocytosis and hypersensitivity reactions
May provoke initial gouty attack
Interacts with aluminum hydroxide, which decreases its absorption
Increases effect of mercaptopurines, cyclophosphamide
Inhibits elimination of chlorpropamide Inhibits metabolism of warfarin, probenecid
Inhibits activation of fluorouracil
Term
Rasburicase
Definition
Urate oxidase found in fungi
Converts uric acid to allantoin, which is highly soluble and eliminated
Foreign protein, high antigenic so only useable once
Used mostly in children
Term
Sumatriptan (Imitrex)
Definition
5-HT receptor agonist
Decreases vasodilation of cerebral arteries
If HA recurs, repeat dose
Expensive
Side effects of vasoconstriction
CI pregnancy, tobacco smoking
Term
Ergotamine tartrate
Definition
Stimulates alpha-1 vasoconstriction and agonist of 5-HT receptors
Most effective, specific for migraines
More vasoconstriction than triptans
Term
Dihydroergotamine
Definition
Same as ergotamine
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