Drugs Block 1 Flashcards
Propanolol
a nonselective beta-adrenergic receptor antagonist; used to tx hypertension, migraines, tremors, and arrhythmia.
Albuterol
a selective β2-adrenergic receptor agonist; bronchodilator used oto tx asthma; receptor activation works to activate downstream adenylate cyclase -→ increase in cAMP which promotes smooth muscle relaxation.
Acetaminophen
NSAID class; antipyretic and analgesic; noncompetitive antagonist (inhibitor) for arachidonic acid at COX1 and COX2; prevents prostaglandin synthesis
Ibuprofen
NSAID class; antipyretic, analgesic and anti-inflammatory; competitive antagonist (inhibitor) for arachidonic acid at COX1 and COX2; prevents prostaglandin synthesis
Ketoprofen
NSAID class; antipyretic, analgesic and anti-inflammatory; competitive antagonist (inhibitor) for arachidonic acid at COX1 and COX2; prevents prostaglandin synthesis; more potent than Ibuprofen
Phenobarbital
a barbiturate; agonist at GABA channel; GABA normally activates Cl- channel, leading to membrane hyperpolarization, and reduced excitability of post-synpatic cell; has anticonvulsant (anti-epileptic) and sedative properties; increases probability of Cl- ch. being open; also directly activates the channel in absence of GABA.
Diazepam
a benzodiazepine; agonist at GABA channel; GABA normally activates Cl- channel, leading to membrane hyperpolarization; reduces excitability of post-synpatic cell; has anticonvulsant and sedative properties; used to tx EtOH withdrawal, anxiety, seizure, spasms, aslo used as sedative for procedures; increases probability of Cl- ch. being open
Gamma hydroxybutyrate
in salt form called sodium oxybate; a CNS depressant used therapeutically to treat narcolepsy and EtOH withdrawal, but also widely abused due to euphoric effects; modulates K+ and Ca+2 channels via GPCR receptors (GABAB and GHB receptor); has a short half-life and low therapeutic index; horrible withdrawal effects (tremor, tachycardia, restlessness, insomnia, anxiety, N/V, delirium, diaphoresis, HTN, coma, and death). Can given pt’s Baclofen (GABAB agonist) to help decrease withdrawal sxs.
Diltiazem
a L-type calcium channel antagonist; used to treat high BP, SVT, angina, vasospasm w/ SAH, and premature labor; reduced Ca entry→smooth muscle relaxation
Nifedipine
a dihydropyridine; L-type calcium channel antagonist; leads to relaxation of vascular smooth muscle; used as antihypertensive
Verapamil
a L-type calcium channel antagonist; used to treat high BP, SVT, angina, vasospasm w/ SAH, and premature labor; reduced Ca entry → smooth muscle relaxation
Erythromycin
antibiotic; also HERG channel antagonist ( K+ ch that repolarizes Vm); leads to prolonged ventricular depolarization and delayed repolarization—Long QT syndrome (predisposition to ventricular arrhythmias)
Sildenafil
inhibits cGMP specific phosphodiesterase Type 5 (PDE5) in smooth muscle; prevents breakdown of cGMP → GMP, thereby preventing muscle relaxation; used to tx erectile dysfunction and pulmonary hypertension;
Minoxidil
K+ channel agonist; influx of K+ will hyperpolarize the membrane potential thus preventing ctxn and promoting relaxation of vascular smooth muscle; used as an antihypertensive and to treat male/female pattern hair loss.
Diazoxide
K+ channel agonist; blocks insulin release from pancreas, also has extrapancreatic (catecholamine-induced) effect used to treat hypoglycemia (due to hyperinsulinemia); also an arteriole vasodilator used to tx malignant HTN
Glibenclamide
a sulfonylurea; antagonist for KATP channels; leads to depolarization of islet cells and subsequent release of insulin; used to tx Type 2 DM.
Glipizide
a sulfonylurea; antagonist for KATP channels; leads to depolarization of islet cells and subsequent release of insulin; used to tx Type 2 DM.
Tolbutamide
a sulfonylurea; direct antagonist for KATP channels in absence of ATP; leads to depolarization of islet cells and subsequent release of insulin; used to tx Type 2 DM.
Octreotide
a naturally occurring somatostatin analogue; decreases endocrine-secretions; can be used to reduce insulin secretion to treat hyperinsulinemia.
Procaine
aka Novocaine; local anesthetic; gold standard for 50 years; slow onset/short lived (ester linkage); lasts 0.5-1 hr; has maximum dose 3-4X higher than other LA’s. Administered via spinal, infiltration, peripheral nerve block
Tetracaine
aka Pontocaine; local anesthetic used for eye surgery; ester linkage, more lipophilic; duration 1.5-6 hours (relatively long); administered via spinal or topical
Benzacaine
aka Hurricane; local anesthetic used in anesthetizing surfaces (topical route); major component of Cetacaine topical spray; not water soluble, no tertiary amine—acts only as un-ionized drug; duration 0.5-1 hr; 20% conc. (very high)
Cocaine
local anesthetic, clinically useful, but abuse liability and cardiotoxicity; ester linkage (slower onset, short-lived), duration 0.5-1 hr; administered topically
Albert Niemann, German chemist first to isolate cocaine. William Halsted, American surgeon who popularized used of cocaine in anesthesia, also an addict.
Lidocaine
aka Xylocaine; a Na+ channel antagonist, used as local anesthetic for dermatological lacerations (also intubations); 30% in un-ionized form; amide linkage (faster onset, longer lasting); duration 0.75-2 hrs; used to block nerve conduction or lower concentration to treat VT in ischemic heart. Administered in all routes (except orally).
Bupivacaine
aka Marcaine; local anesthetic used in obstetrics as epidural; also for local infiltration, peripheral nerve block, IV regional, and topical; has amide linkage (fast onset, long lasting), duration 0.5-8 hours; hydrolyzed by esterases and amidases; most lipophilic (more potent)
Nicotine
agonist of nicotinic receptor in ganglia; affects CV system by elevating BP and HR; also affects CNS (EEG arousal to decreased muscle tone, convulsions).
Succinylcholine
nAChr agonist that causes transient depolarization, followed by desensitization of ACh channels; keeps EPP depolarized as long as it is bound to nAChr (and not broken down by AChE, so long-lasting) thereby inactivating surrounding sodium channels, which cannot recover till EPP repolarizes. Used as a depolarizing block, often in emergent intubating due to fast onset of paralysis.
Varenicline
aka Chantix; partial agonist of nAChR; primary effects are CNS, used for smoking cessation.
Rocuronium
competitive antagonist of nicotinic-ACh receptor; used to produce non-depolarizing block (muscle paralysis) during surgery
Cisatracurium
a competitive antagonist of nicotinic-ACh receptor; used to produce non-depolarizing block (muscle paralysis) during surgery; metabolized differently than rocuronium.
Trimethaphan
a short acting antagonist of ganglionic nicotinic receptors; blocks transmission in parasympathetic and sympathetic ganglia; used for hypertensive emergencies and autonomic testing.
Edrophonium
aka Tensilon; anticholinesterase used to improve eye muscle strength/control in MG patients; also used to dx MG.
Neostigmine
anticholinesterase used to tx MG and to reverse neuromuscular blocks; binds to AChE via esteratic and anionic sites
Pyridostigmine
prophylactic tx for anticholinesterase nerve agents; used by soldiers in areas with high risk of chemical weapons attacks. Also used commonly for maintenance in myasthenia gravis.
Sarin
typical organophosphate anticholinesterase, binds esteratic site via PO43-
Malathione
thiophosphate insecticide, used in humans to tx head lice; generally safe because even though malathion (inactive form) gets converted to malaoxon (active form) by desulfuration, malaoxon is hydrolyzed (inactivated) even more quickly, so there is no build up of active product.
Atropine
PRIMARY tx for anticholinersterase nerve agents
Acetylcholine
agonist of nicotinic acetylcholine receptors; NT for skeletal muscle motor efferents
Pralidoxime
2nd line treatment for organophosphate toxicity
Tetrodotoxin
aka TTX; voltage-gated Na+ channel inhibitor
Botulium toxin
aka Botox; blocks Ca2+ mediated exocytosis of ACh into synaptic cleft; FDA approved to tx muscle spasms
Tetraethylammonium
aka TEA; inhibits voltage-gated K+ channels
