Pharm Flashcards
Blocks ACh-H+ antiporter (STORAGE of ACh) into vesicles
Vesamicol
Prevents UPTAKE of CHOLINE for ACh synthesis
Hemicholinium-3
Degrades synaptobrevin (snap-25), thus preventing the vesicle fusion with presynaptic membrane/inhibiting RELEASE of ACh
Botulinum Toxin
Botulinum Toxin tx:
Dystonias, torticollis, achalasia, strabismus, blepharospasm, pain syndromes, wrinkles, hyperhidrosis
Agent used for diagnosis of MG, eaton-lambert, muscle weakness
Edrophonium
Agents used for urinary or G.I. motility, glaucoma, or NMJ diseases (I.e. MG)
Neostigmine, pyridostigmine, ambenonium
It’s nonpolar/lipophilic structure makes this agent the DOC for tx of CNS anticholinergic toxicity
Physostigmine
These inhibitors of ACh degradation are used to tx Alzheimer’s and Dementia
Tacrine, donepezil, rivastigmine (“pseudo irreversible”), galantamine
Agent used for diagnosis of asthma
Methacholine
Muscarinic receptor agonist for tx of glaucoma
Carbachol
Muscarinic receptor agonist as urinary tract motility agent
Bethanechol
Muscarinic receptor agonists used for Xerostomia in Sjögren’s syndrome
Cevimeline, pilocarpine
Nicotinic receptor agonist used for DEPOLARIZING nm blockade and intubation
Succinylcholine
Muscarinic receptor antagonist used for anticholinesterase overdose, acute bradycardia, mushroom poisoning antidote, mydriasis/opth exam,excessive salivation/mucus during surgery
Atropine
Muscarinic receptor antagonist for N&V and MOTION SICKNESS
Scopolamine
Muscarinic receptor antagonists used for PUD
Pirenzepine, methscopolamine, glycopyrrolate
Muscarinic receptor antagonist used to surgically/vagally induce bradycardia
Glycopyrrolate
Muscarinic receptor antagonists for COPD and asthma
Ipratropium and tiotropium
Muscarinic receptor antagonists used for hyperreflexic/overactive bladder and urge incontinence
Oxybutynin, propantheline, terodiline, tolterodine, fesoterodine, darifenacin, solifenacin, trospium
Nicotinic receptor antagonists for NONDEPOLARIZING nm blockade and intubation: long acting? Intermediate acting? Short acting?
Pancuronium, tubocurarine. Vecuronium, rocuronium. Mivacurium
These Nicotinic receptor antagonists tx HTN in pts with acute aortic dissection
Trimethaphan, mecamylamine
Tx of Pheochromocytoma-assoc. HTN by inhibiting tyrosine hydroxylase, thus inhibiting catecholamine synthesis
Alpha-Methyltyrosine
This agent inhibits catecholamine storage in vesicles by inhibiting VMAT. Used for HTN, common SE is psychotic depression.
Reserpine
These agents inhibit catecholamine storage by concentrating in vesicles and displacing NE. Used to tx HTN.
Guanethidine, guanadrel
Amphetamine and methylphenidate displace catecholamines from storage vesicles, inhibit MAO, and block catecholamine reuptake by NET and DAT. What are their clinical applications?
ADHD, narcolepsy (amphetamine only)
Inhibitor of catecholamine storage, for tx of allergic rhinitis and nasal congestion
Pseudoephedrine
Agent for local anesthesia and Dx of Horners syndrome pupil. Causes marked vasoconstriction and is cardiotoxic
Cocaine
Clinical applications of amitryptiline and imipramine?
OCD, depression, nocturnal enuresis (imipramine)
These MAO inhibitors block catecholamine degradation, tx Depression, and have common SE of tyramine toxicity
Phenelzine, iproniazid, tranylcypromine, clorgyline, selegiline, brofaromine, befloxatone, moclobemide
Alpha1 adrenergic antagonists increase what?
Peripheral vascular resistance, BP
Alpha1 agonist to tx hypotension and shock
Methoxamine
Phenylephrine, oxymetazoline, and tetrahydrozoline are alpha1 agonists that tx??
Ophthalmic hyperemia, nasal congestion, and hypotension(phenylephrine only)
Alpha2 adrenergic agonists inhibit what?
Inhibit sympathetic outflow from CNS, which decreases BP
DOC for tx of HTN during pregnancy
Methyldopa
Alpha2 agonist that txs opioid withdrawal and CA pain?
Clonidine
Alpha2 agonist that’s used for sedation of surgical/ICU pts
Dexmedetomidine
Common SE’s of methyldopa
Hepatotoxicity and hemolytic anemia
Alpha2 agonists that tx HTN
Clonidine, methyldopa, dexmedetomidine, guanabenz, guanfacine
These Beta-adrenergic agonists are BRONCHODILATORS used to tx COPD/asthma
Isoproterenol, dobutamine, metaproterenol, terbutaline, albuterol, salmeterol
Alpha ANTAGONISTS cause
Vasodilation, decreased BP and peripheral resistance
Alpha antagonists that tx Pheochromocytoma-assoc. HTN and sweating
Phenoxybenzamine, phentolamine
Alpha antagonists that tx HTN & BPH. SE is first dose orthostatic hypotension and reflex tachycardia.
Prazosin, terazosin, doxazosin
Alpha1A selective antagonist to tx BPH
Tamsulosin
Alpha2 selective antagonist to tx organic/psychogenic impotence
Yohimbine
Beta-adrenergic antagonists (BETA BLOCKERS) tx
HTN, angina, heart failure
Beta blocker with SE of sedation and decreased libido
Propranolol
Beta blocker to tx glaucoma
Timolol
Beta blocker that requires LFTs bc SE is hepatotoxicity
Labetalol
Beta blocker that is preferred in hypertensive pts who have bradycardia or decreased cardiac reserve
Pindolol
Beta blocker to tx thyroid storm
Esmolol
Nitrate txment of diffuse esophageal spasm
Isosorbide dinitrate
Nitrate for angina prophylaxis and chronic IHD. Not susceptible to first pass metabolism in liver. Less rebound angina SE.
Isosorbide 5-mononitrate
IV tx of unstable angina or acute heart failure
nitroglycerin
Avoid co-administration with phosphodiesterase V inhibitors (sildenafil, etc)
Nitrates
Nitrate for hypertensive emergencies, severe cardiac failure, and ergot alkaloid toxicity. SE’s are cyanide toxicity, methemoglobinemia, increase ICP, etc.
Sodium nitroprusside
Tx for neonatal respiratory failure, perinatal hypoxia, and pulmonary hypertension
Inhaled NO gas
Phosphodiesterase type V inhibitors cause an increase in what?
cGMP
PDE5 inhibitors for erectile dysfunction
Sildenafil (also tx pulmonary HTN), vardenafil, tadalafil (longer elimination half life)
CCB that tx exertional angina,unstable angina,coronary spasm, hypertension,hypertrophic cardiomyopathy, Reynauds phenomenon, pre-eclampsia
Nifedipine, amlodipine, felodipine, clevidipine
CCB that can cause a brisk fall in BP, triggering sever reflex tachycardia
Nifedipine
CCB administered IV for hypertensive urgency/emergency
Clevidipine
CCBs for tx of prinzmetal angina, chronic stable angina, HTN, atrial fibrillation or flutter, PSVT
Diltiazem, Verapamil
K+ channel openers for tx of severe/refractory HTN
Minoxidil, pinacidil, nicorandil, cromakalim
K+ channel opener for male pattern alopecia
Minoxidil
Endothelin receptor antagonists for sever pulmonary HTN. Must monitor LFTs. Pregnancy is contraindication.
Bosentan, ambrisentan
ET receptor with greater selectivity for ETa
Ambrisentan
Arteriolar vasodilator to tx severe HTN/heart failure. SE’s are agranulocytosis, hepatotoxicity, lupus like syndrome
Hydralazine
ACE inhibitors
Captopril, enalapril, lisinopril
ACE inhibitor SE’s??
Cough, angioedema, hyperkalemia
ACE Inhibitor administered as active drug and processed to active metabolite
Captopril
ACE inhibitor that’s an ester prodrug converted to active metabolite in plasma
Enalapril
ACE inhibitor administered as active drug and excreted unchanged
Lisinopril
AT1 receptor antagonists for tx of HTN, diabetic nephropathy, heart failure, MI, stroke
Losartan, valsartan
NA channel inhibitor for tx of status epilepticus, seizures related to eclampsia, arrhythmias
Phenytoin
NA channel inhibitor for tx of bipolar disorder, trigeminal neuralgia
Carbamezine
NA channel inhibitor for tx of bipolar disorder, atypical absence seizures
Lamotrigine