Pharmacology Flashcards
Bethanechol (Urecholine)
- direct acting carbamic ester
- direct acting muscarinic cholinomimetic
- used for post op and neurogenic ileus, urinary retention
- side effects: SLUDGE
Muscarine
Pilocarpine (Salagen)
Cevimeline (Evoxac)
- direct acting non-ester alkaloid
- direct acting muscarinic cholinomimetic
- side effects: SLUDGE
- pilocarpine: treats glaucoa
- cevimeline: treats dry mouth
Nicotine (NRT)
- direct acting non-ester alkoloid
- direct acting nicotinic cholinomimetic
- used for smoking cessation (reduces cravings)
short acting AChE inhibitors (0.5-2 hrs)
- indirect acting carbamates; dock like ACh to temporarily inhibit
- side effects: SLUDGE, general increase in cholinergic neurotransmission; paralysis
- neostigmine (prostigmin): post operative and neurogenic ileus, urinary retension, myasthenia gravis, reversal of neuromuscular blockade
- physostigmine (eserine): treats glaucoma
Donepezil (Aricept)
- indirect acting non-ester
- AChE inhibitor
- treats Alzheimer’s (amplifies endogenous ACh in brain)
- side effects: SLUDGE, general increase in cholinergic neurotransmission, paralysis
Edrophonium (Enlon)
- indirect active non-ester
- AChE inhibitor (v. short acting 5-15mins)
- used to diagnose myasthenia gravis (deficiency vs. ACh crisis); treats ileus
- side effects: SLUDGE, general increase in cholinergic neurotransmission, paralysis
Echothiophate (Phospholine)
- indirect acting organophosphate
- long acting ACh inhibitor (>100 hrs)
- treats glaucoma
- side effects: SLUDGE, general increase in cholinergic neurotransmission, paralysis
Pralidoxine (Protopam)
- strong nucleophile that regenerates phosphorylated AChE
- treats poisoning by nerve gas, insecticide; give for overdose of any indirect acting muscarinic
Sarin
Parathion
- very potent indirect acting organophosphate
- AChE inhibitor (forms covalent bond with receptor)
- side effects: SLUDGE, general increase in cholinergic neurotransmission, paralysis; death
- treat with pralidoxime and atropine before aging
- sarin: volatile nerve gas
- parathion: insecticide
tertiary amine antimuscarinics
- block muscarinic receptors
- side effects: general block of muscarinic functions
- atropine: mydriasis, cycloplegia
- scoploamine: prevent/reduce motion sickness
- tropicamine: myrdiasis, clycloplegia (rapidly metabolized)
- tolterodine (detrol): transient cystits, post op bladder spasms, incontinence
- benztropine: treat maniestations of parkinson’s (crosses BBB)
quaternary amine antimuscarinic
- blocks muscarinic receptors
- side effects: general block of muscarinic functions
- glycopyrrolate: reduces transient hypermotility (crosses membranes poorly)
- ipratropium (atrovent): bronchodilation in asthma/COPD
- tiotropium (spiriva): bronchodilation in asthma/COPD; longer acting that ipratropium
Hexamethoium (Methium)
Mecamylamine
- ganglionic blocker; competitively inhibits Nn receptor and sympathetic tone
- treats: HTN crisis; “bloodless” field surgery
- rarely used
Succinylcholine (Anectine)
- depolarizing blocker (MC used); overstimulates N receptor→ desensitization of muscle unit to further ACh (flaccid paralysis in 1 min)
- used for brief procedures (tracheal intubation, dislocation resets)
- side effects: respiratory paralysis, disturbance of autonomic function
Tubocurarine (Curare)
Mivacurium (Mivacron)
- nondepolarizing blocker; blocks nicotinic (Nm) receptor
- muscle relaxant or surgery without deep anesthesia
- side effects: respiratory paralysis, disturbance of autonomic function
- tubocurarine: lasts 30-60 mins
- mivacurium: short acting (rapidly hydrolyzed)
Botulinum A toxin (Botox)
- local paralytic; blocks vesicle fusion and ACh release on presynaptic terminal by degrading SNAP-25
- treats achalasia, strabismus, oromandibular dystonia; reduces wrinkles
hyperbaric oxygen
- prevents lipid peroxidation and delayed nerologic sequelae in CO poisoning
- use in high risk individuals after smoke inhalation ( >30 y.o and/or loss of consciousness)
nitrites
- turns RBC Hb→ metHb, CN moves Fe3+ on cyt to those in RBCs creating cyanometHb
- dangerous for use with concurrent CO poisoning
- patients who are G6PD deficiency will not respond to this treatment
sodium thiosulfate
enhances normal metabolism of cyanide via rhodanase
hydroxycobalamin (cyanokit)
- binds with cyanide→ cyanocobalamin (B12)
- treats smoke inhalation victims not improving with supportive care; cyanide exposure; nitroprusside at risk patients
- give concurrently with sodium thiosulfate
methylene blue (urolene blue)
- cofactor of NADPH reductase (gains e and donates it to reduce metHb)
- treats methemoglobinemia >20-30% or with symptoms
- side effects: hemolytic anemia (weak oxidizing capability); pain at injection site, dyspnea, reslessness, tremor
norepi (levophed)
- nonselective agonist; α1, α2, β1
- treats acute hypertension
- side effects: HTN, arrythmias, headache
epi
- neurohormone (no synapse)
- nonselective agonist; α1, (α2), β1, β2
- treats anaphylactic shock; + local anesthetics for dental procedures (less dramatic effect on BP, less irritating, and more potent than NE); glaucoma
- side effects: palpitations, arrythmias, headache
amphetamine
- indirect acting (increases release of norepi)
- treats ADHD, narcolepsy; just for funsies
- side effects: HTN, insomnia, anxiety, arrythmias
isoproterenol
- nonselective β agonist (β1, β2)
- treats shock, heart block
- side effects: palpitation, tachy, headache
dobutamine
- β1-selective agonist
- treats cardiac decompensation, shock, heart block; used as chemical cardiac stress test
- side effects: tachyarrythmias, HTN
albuterol (proventil)
terbutaline (brethine)
- β2-selective agonist
- prevents/reverses exercise-induced bronchospasm; treats mild asthma, COPD
- terbutaline: treats early labor
- side effects: can mask progressively severe inflammation; tachycardia, muscle tremor
- takes 10-15 mins to act with 6-12 hrs duration
- nebulizer delivers more but there are greater side effects; oral is least effective (requires more dose→ side effects)
phenylephrine (neo-synephrine)
- α1-selective agonist
- treats nasal congestion, posterural hypotension
- side effects: HTN, reflex brady; desensitize receptors with overuse→ rebound congestion
clonidine (catapres)
- α2-selective agonist (CNS)
- treats HTN, shock, withdrawal from drug dependence
- side effects: sedation
α-methyldopa (Aldomet)
- prodrug crosses BBB, metabolite (a-methylnorepi) activates CNS α2
- treats HTN
- side effects: sedation
fenoldopam (corlopam)
- selective dopamine agonist (D1 only)
- increases blood flow at renal, mesenteric, and cerebral arteries
- 10 min half life (good for HTN emergencies)
dopamine
- mixed acting (direct/indirect) agonist: D1, α1, β1
- Low dose: direct @ D1; treats renal failure
- Medium dose: direct @ β1, some indirect; treats shock
- High dose: direct @ α1, some indirect; vasoconstriction (treats HTN)
phentolamine (regitine)
phenoxybenzamine (dibenzyline)
- nonselective α-antagonists
- treats pheochromocytoma (during surgery because trauma→ high catecholamines), Raynaud’s, frostbite
- side effects: postural hypotension, inhibits ejaculaton
- phenoxybenzamine: also is a non-competitve blocker (covalently bonds to receptors)
prazosin (minipress)
terazosin (hytrin)
- α1-selective antagonists
- treats primary HTN, BPH (decrease resistance to urine outflow)
- side effects: postural hypotension (usually 1st dose); less side effects than the nonselective α antagonists
1st generation nonselective β-antagonist
- propranolol (inderal): angina, HTN, arrythmias, migrains, anxiety
- timolol (betimol): glaucoma
- side effects: bradycardia, bronchoconstriction, sexual dysfunction
- do not use for CHF