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83 Cards in this Set
- Front
- Back
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Terfenadine
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prodrug --> H-1 histamine receptor antagonist
CYP3A4 - competes with erythromycin, tetracycline |
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Warfarin
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Anticoagulant - VKORC1
CYP2C9, displaced by phenylbutazone |
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Guanethidine
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antihypertensive - blocks catecholamine transport into vesicle; inhibits adrenergic vesicle release; does NOT cross BBB
Uses uptake-1 --> minor competitive inhibition of uptake SE: diarrhea, retrograde ejaculation, orthostatic hypotension |
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Guanadrel
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antihypertensive - blocks catecholamine transport into vesicle; inhibits adrenergic vesicle release; does not cross BBB; short half-life
Uses uptake-1 --> minor competitive inhibition of uptake less SE than guanethidine |
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Reserpine
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Antihypertensive - depletes catecholemine vesicular stores of NE; blocks vesicular membrane amine-hydrogen antiport; crosses BBB
SE: severe depression, GI hemorrhage (due to histamine release) |
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Tyramine
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Displaces catecholamines from presynaptic terminals
Competitive inhibitor of uptake-1 Similar to amphetamine but degraded by MAO |
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Metyrosine
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Competitive inhibitor of TH (RLS of catecholamine synthesis)
Treatment of pheochromocytomas SE: crystalluria, hematuria |
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Carbidopa
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AAAD inhibitor; does not cross BBB; used with L-Dopa and COMT inhibitors to treat Parkinson's disease
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Disulfiram (Antabuse)
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DBH inhibitor; copper chelator; Tx of alcoholics (inhibits aldehyde dehydrogenase)
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SKF-64139 and SKF-7698
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PNMT inhibitors; not in clinical practice
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Cocaine
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alkaloid; inhibits neural membrane uptake of catecholamines; crosses BBB
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Nitecapone
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COMT inhibitor; used with L-dopa and carbidopa in Tx of Parkinson's disease
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Tolcapone
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COMT inhibitor; used with L-dopa and carbidopa in Tx of Parkinson's disease
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Chlorgyline
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MAO A inhibitor; antidepressant
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Deprenyl
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MAO B inhibitor; Tx for MPTP-induced Parkinson's disease
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Norepinephrine
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Alpha agonist; beta-1 agonist
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Epinephrine
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Alpha and beta agonist
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Alpha-methylnorepinephrine
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Alpha-2 agonist; antihypertensive
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Clonidine
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Alpha-2 agonist; antihypertensive
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Prazosin
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Alpha-1 antagonist
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Isoproterenol
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Beta agonist
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Phenylephrine
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Alpha agonist; NOT a COMT substrate
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Methoxamine
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Alpha agonist; NOT a COMT substrate
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Dobutamine
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Beta-1 agonist; Tx for CHF
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Terbutaline
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Beta-2 agonist; bronchodilator
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Albuterol
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Beta-2 agonist; Tx for asthma
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Phenoxybenzamine
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Alpha antagonist; blocks uptake 1, uptake 2, and alpha receptor; Tx of pheocromocytoma; long half-life (24 hr)
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Phentolamine
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Alpha antagonist; short half-life; used in OR
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Prazosin
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Alpha-1 antagonist
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Yohimbine
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Alpha-2 antagonist
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Dichloroisoproterenol (DCI)
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Beta antagonist
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Propranolol
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Beta antagonist
SE: bronchospasm in asthma patients, atrio-ventricular block, aggravation of peripheral arterial vascular disease |
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Atenolol
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Beta-1 antagonist
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Metoprolol
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Beta-1 antagonist
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Hemicholinium
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Inhibits Na/choline symporter (experimental)
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Vesamicol
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Inhibits ACh/H+ antiporter (vesicle) (experimental)
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3,4-diaminopyridine
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Stimulates cholinergic vesicle fusion; Tx for Lambert-Eaton myasthenic syndrome
SE: mild paresthesias |
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Latrotoxin (black widow venom) and Beta Bungarotoxin (tropical snake venom)
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Destroys ACh synaptic vesicles --> flooding of ACh and synaptic failure
Localized diaphoresis, weakness, parestheias CV collapse, pulmonary edema, ileus |
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Botulinum toxin
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Inhibits cholinergic vesicle fusion; local Tx for spastic disorders
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Acetylcholine
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Cholinergic agonist (degraded too rapidly for clinical use)
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Bethanechol
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Muscarinic agonist; resistant to AChE; bowl and bladder
SE: SLUDGE |
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Carbachol
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Muscarinic and nicotinic agonist; resistant to AChE (experimental)
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Pilocarpine
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Muscarinic agonist; very stable; used for glaucoma
SE: CNS disturbances; profuse sweating |
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Atropine
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Muscarinic antagonist; lasts 4 hrs (days in eye)
Tx for mydriasis, spasmodic bladder/GI, cholindergic overdose; preop antisecretory agent SE: "dry as a bone" etc. etc. |
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Scoplamine
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Muscarinic antagonist; stronger CNS, short term memory loss; Tx for motion sickness
SE: "dry as a bone" etc. etc. |
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Curare
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Nicotinic (Neuromuscular) antagonist
Tubocurarine, pancuronium, vecuronium, atracurium |
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Succinylcholine
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Nicotinic (Neuromuscular) antagonist; short action
Resists degradation by AChE Phase I - depolarization Phase II - inactivated channels SE: Malignant hyperthermia with halothane, apnea |
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Edrophonium
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Anticholinesterase; short acting; used for Dx of myasthenia gravis
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Neostigmine
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Anticholinesterase; medium acting; Tx for MG
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Pyridostigmine
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Anti-cholinesterase; medium acting; topical tx of glaucoma
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Pralidoxime
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Rescues AChE from organophosphates (before aging)
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Adenosine
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Purinergic agonist; stimulates IKACh; Tx for SVT
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Carbamazepine
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Anti-convulsant (simple/complex partial, tonic-clonic), blocks Na channels (use-dependent), induces and metabolized by CYP3A4
Also used for headache, pain, and psychiatric disease (mood stabilizer) SE: leukopenia, diplopia, osteoporosis, reduced hormonal efficacy |
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Phenobarbital
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Anti-convulsant (recurrent, febrile, simple partial (alt), tonic-clonic (alt), status epilepticus (alt)), enhance GABA inhibition (increases DURATION of GABA-A receptor opening), induces P450
SE: sedation, cognitive decline, osteoporosis, reduced hormonal efficacy |
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Phenytoin
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Anti-convulsant (simple/complex partial, tonic-clonic, status epilepticus), blocks Na channels (use-dependent), also antiarrhythmic, induces and is metabolized by P450, highly bound to albumin (risk for competing drugs)
SE: hirsuitism, neuropathy, ataxia, gingival hyperplasia, teratogenic, osteoporosis, reduced hormonal efficacy |
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Valproate
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Anti-convulsant (myoclonic, absence (alt), tonic-clonic (alt)), blocks Na (use-dependent) and Ca (T-type) channels, also used for headache, pain, and psychiatric disease (mood stabilizer), 90% bound to plasma protein, metabolized by P450 (does not induce), widely used, safe for pediatrics
SE: (low frequency of SE) teratogenic, weight gain, tremor, polycystic ovaries, anovulatory cycles, encephalopathy, osteoporosis |
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Felbamate
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Anti-convulsant (partial or generalized), enhances GABA inhibition, blocks glutamate receptor binding
SE: reduced hormonal efficacy |
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Gabapentin
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Antil-convulsant (partial), GABA analog but doesn't react with GABA receptors, may block Ca channels (L-type)
Also used for headache, pain, not metabolized in liver --> can use with liver disease, no known drug interactions SE: + or - weight gain, neurotoxicity (dizziness or drowsiness) |
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Lamotrigine
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Anti-convulsant (partial or generalized), blocks Na (use-dependent) and Ca channels, also used for psychiatric disease (mood stabilizer)
SE: rash, drug interactions, headache, (good SE profile for pregnacy |
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Levetiracetam
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Anti-convulsant (partial or generalized), unknown mechanism, not metabolized in liver --> can use with liver disease, no known drug interactions
SE: drowsiness, irritability |
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Oxcarbazepine
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Anti-convulsant (partial), blocks Na channels (use-dependent)
SE: hyponatremia, neurotoxicity, drug interactions, rash, reduced hormonal efficacy |
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Trigabine
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Anti-convulsant (partial)
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Topiramate
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Anti-convulsant (partial or generalized), blocks Na (use-dependent) and Ca (L-type) channels, enhances GABA inhibition (increases FREQUENCY of Cl channel opening), blocks glutamate receptor binding
Also used for migraine, headache, pain, obesity, and psychiatric disease (mood stabilizer) SE: weight loss, cognitive (memory loss - due to glutamate blocking), kidney stones, glaucoma, increases phenytoin level, sulfamate (pts allergic to sulfa drugs), reduced hormonal efficacy |
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Zonisamide
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Anti-convulsant (partial or generalized (?)), blocks Na (use-dependent) and Ca (T-type) channels, enhances GABA inhibition, also used for obesity
SE: oligohydrosis, stones, weight loss, behavior, sulfonamide (pts allergic to sulfa drugs) |
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Pregabalin
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Anti-convulsant (partial), binds Ca channels,
Also used for headache, pain, and psychiatric disease (mood stabilizer), not metabolized in liver --> can use with liver disease, no known drug interactions SE: weight gain, mild neurotoxicity |
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Benzodiazepines
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Anti-convulsant, enhance GABA inhibition (increasing the FREQUENCY of GABA-A receptor Cl channel opening)
Safest, most free of severe side effects of all AEDs SE: sedation |
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Clonazepam (Benzodiazepine)
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Anti-convulsant (absence, myoclonic), chronic treatment
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Clorazepate (Benzodiazepine)
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Anti-convulsant (partial), chronic treatment, used with other drugs
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Diazepam/Lorazepam (Benzodiazepine)
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Anti-convulsant (repetitive, status epilepticus), acute treatment ("fire extinguisher"), lorazepam-longer duration
SE: sedation, memory |
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Ethosuximide
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Anti-convulsant (absence), T-type Ca current suppressor
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Cholestyramine
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Ion exchange resin, bines corticosteroids, thyroxine, and digitalis --> inhibits absorption
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Doxorubicin
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Chemotherapy, binds to DNA (anthracycline), cardiotoxicity
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Lacosamide
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Anti-convulsant (partial)
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Rufinamide
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(New) Anti-convulsant (generalized), Lennox-Gastaut syndrome
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Vigabatrin
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Anti-convulsant (infantile spasms) inhibits GABA transaminase,
SE: visual field abnormalities |
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Tricyclic Antidepressants
(Amitripyline, Nortriptyline, Doxepin, Clomipramine, Imipramine, Desiprimine) |
NE & serotonin reuptake inhibition
SE: muscarinic blockade (blurred vision, dry mouth, urinary retention, constipation, narrow angle, glaucoma), alpha-adrenergic (orthostatic hypotension, dizziness, tachycardia), cardiac arrest, confusion in elderly |
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MAOI Antidepressants (Isocarboxazid, Phenelzine, Tranylcypromine)
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Increased tyramine (from aged, fermented foods)
SE: orthostatic hypotension, insomnia, hypertensive crises (tachycardia, headache, stiff neck, arrhythmia, seizure, stroke) |
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SSRIs (Citralopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline)
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Depression, panic disorder, GAD, OCD, social phobia, PTSD, bulimia nervosa
Metabolized by and inhibits P450 (2D6) SE: GI (nausea, vomiting, diarrhea), sexual dysfunction, "anxiety", sleep disturbance, headache, sucidial ideation (?), serotonin toxicity |
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SNRI (Duloxetine, Venlafaxine, Desmethylvenlafaxine)
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Venlafaxine: depression, GAD, panic disorder, social phobia
Duloxetine: depression, GAD, diabetic neuropathy, fibromyalgia SE: nausea, insomnia, headaches, hypertension, sexual dysfunction |
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Bupropion
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Atypical antidepressant, dopamine & NE reuptake inhibitor, depression, smoking cessation
SE: seizure risk, (less) sexual dysfunction |
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Mirtazapine
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atypical antidepressant, blocks presynaptic alpha-2 receptors, antihistamine activity
SE: sedation, weight gain |
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Nefazodone
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Atypical antidepressant, not used much anymore
SE: hepatotoxicity |
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Trazadone
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Atypical antidepressant, hypnotic
SE: priapism |
