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86 Cards in this Set
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sildenafil
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(viagra) Inhibits cGMP PDE 5. PDE-5 breaks down cGMP in Corpus cavernosum. So more cGMP is available, pronounced vasodilation. Short T1/2 ~4 hours
Side effects: General vasodilation, increase heart rate, visual issues (blue/green discrimination), auditory issues. Drug Interactions: Drugs metabolized by CYP3A4 (erythromycin, cimetidine, ketoconazole) |
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tadalafil
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(cialis) same as sildenafil. cGMP more available to vascular smooth muscle due to inhibition of PDE-5. T1/2 is ~36 hours
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vardenafil
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(levitra) same as sildenafil.
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BOTOX
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Botunlinium toxin, Clostridium botulinium. Prevents release of ACh from nerve endings.
Tx dystonia, wrinkles, excessive sweating etc.. |
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atropine
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
hyoscyamine ↑Cardiac stimulation ↓Glandular Secretion (saliva, etc. important for dental) |
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scopolamine / methscopolamine
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
hyoscine TX of motion sickness and vertigo. CNS sedation |
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dicyclomine
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
bentyl anti-spasmodic for Tx of IBS |
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propantheline
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
Antispasmodic for Tx of IBS |
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glycopyrrolate
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
PRE OP drug robinul ↓Saliva (important for dental procedures) and ↓vagal reflexes |
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ipratropium
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
Atrovent COPD and Asthma. ↑ Bronchodilation. Shorter action than tiatropium |
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tiatropium
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
Spiriva COPD and Asthma. Long term action in comparison to ipratropium ↑Bronchodilation |
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benztropine
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
congentin Parkinson's (also benedryl for Parkinson's) |
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trihexyphendiyl
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
Artane Parkinson's (also diphenhydramine for Parkinson's) |
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tolterodine
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
detrol Tx of Urinary incontinence |
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oxybutynin
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
ditropan Tx of Urinary incontinence |
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solifenacin
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
Vesicare Tx of Urinary incontinence |
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tropicamide
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Anticholinergic/Muscarinic Antagonist (↑ Sympathetic response/↓ Parasymp)
Mydriacyl Used to dilate pupil (mydriasis) |
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ALL MUSCARINIC ANTAGONISTS
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↓GI Motil / ↑Sphincter tone / ↑Pupil size
Pre-Op - reduce vagal tone on heart, dry saliva/secretions Side Effects: - Dry mouth - dry, hot skin (hyperthermia) - constipation, urine retention - visual issues, blurred vision, photophobia - Sedation, confusion, amnesia Careful with: Glaucoma, prostate hypertrophy, CV unstable, Ulcerative colitis Antidote for AChE inhibitors poisoning. (muscarine mushrooms) Prevent motion sickness. Tx Parkinson's. Cardiac Stimulation (atropine) Asthma and COPD / dry respiratory secretions |
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pancuronium
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A competitive (non-depolarizing) neuromuscular antagonist.
Pavulon Competitive ACh antagonist that produces muscular relaxation. used in combo w/ anesthesia |
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succinylcholine
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Depolarizing neuromuscular antagonist.
Anectine Initially stimulates receptor → weak contractions → relaxation and paralysis. Used in combo w/ anesthesia |
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ABCD
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Alphas Constrict / Betas Dilate
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Epinephrine (E/Epi)
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Nonselective agonist. Stimulates all Alpha and Beta receptors.
Used in circulatory shock, tx bronchospasm and circulatory collapse (anaphylaxis). Tx Bronchoconstriction in asthma (causes reversal). Tx bradycardia with high doses. Mixed with local anesthetic to prolong effect/minimize bleeding (septo with epi) ↑ Systolic Pressure / ↓Diastolic / NC in MAP. ↑in HR |
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Norepinephrine (NE)
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Nonselective Agonist. Stimulation of all Alpha and Beta1 (not as much for Beta2). Used to effect vascular alphas. Used in cardiogenic, neurogenic, septic shock. Supports BP in spinal anesthesia.
Causes ↑ in systolic/diastolic/mean pressures (no change in pulse pressure). ↓ in Heart Rate. |
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Isoproterenol
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Stimulates all Beta but no Alpha.
Not often used clinically, could be used for bronchodilation in asthma. ↑HR / ↓Sys/Dia -- ↑MAP |
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Dopamine (D/DA)
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Non selective agonist. Stimulates Dopamine receptors>B1>A1>>>> others.
↑Blood supply to GI and kidney. Stimulates contractility and HR (b1). Some vasoconstriction (a1). Shock (cardio/neuro/septic). Congestive heart failure and bradycardia. |
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Dobutamine
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Selective B1 agonist. Used to ↑Contractility ↑Cardiac Output/Pulse Pressure. Used in CHF and shock.
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Selective B2 agonists
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AlbuTERol, metaproTERenol, pirbuTERol, salmeTERol, TERbutaline. TER= B2 slective.
Bronchodilation in "rescue" inhalers. Overstimulation can activate B1s too. |
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Phenylephrine/midodrine
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Selective a1 agonist
Used to maintain MAP. Tx of hemorrhoids/congestion (vasoconstriction leads to less swelling). Mydriatic. |
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Cocaine
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Anesthetic. NE reuptake inhibitor.
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pseudoephedrine/ephedrine
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Stimulate release of NE, also can acts as an agonist. Tx of nasal/bronchial congestion
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amphetamine/methamphetamine/metylphenidate
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Stimulates release of catecholamines from axon terminals.
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labetalol
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(trandate) - Combination alpha/beta blocker. TX of extremely high BP. Causes decrease in vasoconstriction and Cardiac output.
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acebutolol
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(sectral) cardiospecific (b1) beta blocker w/ partial agonist and local anesthetic. Low lipid solubility - longer duration of action
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atenolol
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(tenormin) cardiospecific (b1) Beta blocker low lipid solubility - longer duration of action
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esmolol
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(brevibloc) cardiospecific (b1) beta blocker Low lipid solubility - but Exception is Esmolol that is cleared by Esterases SHORT ACTION
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metoprolol
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(lopressor, toprol-XL) cardiospecific (b1) beta blocker w/ local anesthetic. medium lipid solubility - intermediate duration of action
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nadolol
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(corgard) nonselective Beta blocker. low lipid solubility - long term action.
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pindolol
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nonselective Beta blocker. w/ local anesthetic and partial agonist (ISA) activity. medium lipid solubility - intermediate term action.
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propranolol
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(inderal-LA) nonselective Beta blocker. Some local anesthetic action. high lipid solubility - short term action. (Easily crosses CNS → Ataxia)
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timolol
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(timoptic) nonselective Beta blocker. medium lipid solubility - intermediate term action.
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phenoxybenzamine
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(Dibenzyline) non-selective alpha blocker. Irreversibly binds, must make a new receptor. Used in pheochromocytoma pts.
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phentolamine
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(OraVerse) non-selective alpha blocker. Used with pheo pts. Doesn't last as long as phenoxybenzamine. Also used to reverse local anesthetic w/ epi.
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prazosin
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(Minipress) PROTOTYPIC a1 selective blocker. Long term tx of hypertension. Relax urinary smooth muscle, help retention issues.
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terazosin
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(Hytrin) a1 selective blocker. Identical to prazosin w/ longer action.
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doxazosin
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(Cardura) a1 selective blocker. identical to prasozin w/ longer action.
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tamsulosin
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(Flomax) a1 selective blocker. Good for Tx of BPH (benign prostatic hyperplasia/ urinary retention) acts on a1a which are in bladder neck.
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alfuzosin
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(Uroxatral) a1 selective blocker. "uroselective" but not due to a1a like silodosin/tamsulosin, but accumulates in prostate.
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silodosin
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(Rapaflo) a1 selective blocker. Good for Tx of BPH (benign prostatic hyperplasia/ urinary retention) acts on a1a which are in bladder neck.
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reserpine
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Periph-Symp Blocker. Decreases uptake of DA and NE. This overtime reduces amt of NT's released. ↓ BP via ↓CO/↓MAP. Long-term effect due to irreversible depletion of NE vesicles.
Side effects: sedation, postural hypotension, bradycardia, fluid retention. GI issues, diarrhea/ulcers etc.. |
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guanethidine
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(Ismelin) Periph-Symp blocker. Identical to reserpine, without CNS effects, guanethidine cannot cross barrier. Same GI side effects.
DRUG INTERACTION - tricycle antidepressants |
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methyldopa
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Central-Symp Blocker. a2 agonist, ↓symp outflow from CNS (affects pre-synaptic a2).
A 'pro-drug' needs metabolism to be active. MOA - ↓Renin release/↓HR and CO/↓MAP. Tx of hypertension in pregnant Auto-immune side effects: Coombs test + w/o hemolytic anemia and abnormal liver function. Common side effects: dry mouth/fluid retention/sedation |
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clonidine
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(Catapres) Central-Symp Blocker. Smaller dose needed/absorbed through skin (patch) yields long-term hypertensive tx.
Other uses: ADHD/Migraine/hot flashes/PTSD/ drug withdrawal Direct injection of clonidine in spine → analgesic |
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guanfacine
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(Tenex/Intuniv) Central-Symp Blocker. same as clonidine → less sedation/withdrawal and marketed for ADHD
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Nicotine
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Stimulates all Nicotinic receptors. N1 and N2.
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High doses of Nicotine
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Similar to a parasympathetic response. ↓CNS activity (respiration). ↓BP .
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Low doses of Nicotine
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Similar to sympathetic. ↓GI motility. ↑Vasoconstriction. ↑CNS stimulation.
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mecamylamine
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ganglionic blocking agent. (discontinued). used to tx tourette's. Blocks N2 receptors only (no muscular issues). Dangerous because they messed with baroreflexes. Mostly sympathetic response.
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ergotamine tartrate
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(Ergomar) Tx of Migraines via intercranial vasoconstriction. a 5HT activator. Activates DA/Epi/Sero receptors to vasoconstrict.
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dihydroergotamine
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(DHE 45/Migranol - nasal spray) Tx of Migraines via intercranial vasoconstriction. a 5HT activator.
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methysergide maleate
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(Sansert) Ergot alkaloid for Tx of migraines. Serotonin antagonist w/ partial agonist activity.
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sumatriptan
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(Imitrex) Ergot alkaloid for Tx of migraines. A 1st Generation 5HT agonist.
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zolmitriptan
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(Zomig) Ergot alkaloid for Tx of migraines. A 2nd Generation 5HT agonist.
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metoclopramide
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(Reglan) Dopamine antagonist -antiemetic (anti-nausea). A DA antagonist that blocks DA receptors in the CTZ (chemoreceptor trigger zone) - the vomitting center.
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prochlorperazine
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(Compazine) Dopamine antagonist -antiemetic (anti-nausea) and migraine Tx. A DA antagonist that blocks DA receptors in the CTZ (chemoreceptor trigger zone) - the vomitting center.
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midrin
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(Isometheptene (vasoconstriction) /Dichloralphenazone (mild sedative) + Acetominophen) Analgesic. Tx of migraines.
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amitriptyline
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(Elavil) - antidepressant that can Tx Migraines. Serotonin receptor - NE reuptake inhibitor.
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valproate/topiramate/gabapentin
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(Depakote/Topamax/Neurontin) Anti-seizure / Tx of migraines.
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morphine
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Opioid. Strong mu agonist. prototypic, severe pain
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codeine
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Opioid. moderate mu agonist. moderate pain. Anti-tussive
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fentanyl
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Opioid. extremely Strong mu agonist. very potent severe and chronic pain. Transdermal (duragesic)
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heroin
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Opioid. Strong mu agonist. schedule I (not available in US)
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hydrocodone
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Opioid. moderate mu agonist. mild-moderate pain
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hydromorphone
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Opioid. very Strong mu agonist. severe pain
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meperidine
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Opioid. Strong mu agonist. severe pain. Not useful in chronic pain, due to metabolite
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methadone
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Opioid. Strong mu agonist. chronic pain and opioid addicts
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oxycodone
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Opioid. moderate mu agonist. mod- severe pain. "hillbilly heroin"
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oxymorphone
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opioid
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propoxyphene
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Opioid. weak/moderate mu agonist. moderate pain (poor relief). taken off market. high cardiac toxicity.
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pentazocine
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Opioid w/ naloxone. kappa agonist/mu partial. moderate pain relief. Naloxone inactivated if taken properly.
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buprenophine
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Opioid. mu partial agonist (antag at high doses). Out patient -office based- Tx of opioid addiction.
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butorphanol
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similar to pentazocine.
Opioid w/ naloxone. kappa agonist/mu partial. moderate pain relief. Naloxone inactivated if taken properly. |
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tramadol
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opioid. weak mu agonist/NE and Serotonin reuptake inhibitor. This enhances pain relief.
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naloxone
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Opioid Antagonist. used for Opioid poisoning, will illicit withdrawal effects. Parenterally only.
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naltrexone
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Opioid antagonist. long half life, effective with providers who once abused opioids. "immunizing effect"
Also quite effective with Alcoholics |
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methlynaltrexone
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Quat. Salt of naltrexone. Opioid Antagonist. Parenterally only.
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alvimopan
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similar to methylnaltrexone. Opioid Antagonist. more orally effective.
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