MOD II 2.3 Final

parasympathetic function, NT, receptors? sympathetic function, NT, receptors?

• rest + digest, ACh (pre/postganglionic)

  • muscarinic → M1-M5 (GPCR)

• fight or flight, ACh (preganglionic) + NE (postganglionic)

  • adrenergic → a1, a2, B1, B2 (GPCR)

  • nicotinic → ion channels

varenicline MOA, indication, adverse effect?

• nicotinic agonist, partial

• smoking cessation + dry eye syndrome

• vivid dreams, angioedema, hypersensitivity rxn

succinylcholine MOA, indication, adverse effect? drug interaction?

• nicotinic agonist, full

• blocks N-MSK depolarization → skeletal muscle relaxation during intubation

• hyperkalemia + malignant hyperthemia

  • rocuronium (nicotinic antagonist) = muscle relax

bethanechol, pilocarpine, methacholine MOA, indication, adverse effect?

• muscarinic agonist (cholinergic agents)

• B: urinary retention, M: asthma, P: dry mouth

• AE: DUMBBELSS + CI: mechanical obstruction

atropine MOA? indication? AE, CI?

• muscarinic antagonist (anticholinergic)

• bradycardia (AV block), reduce DUMBBELSS, anticholinesterase poisoning

• AE: mydriasis, blurry vision, dry mouth (xerostoma); CI: glaucoma, BPH, pyloric stenosis

ipratropium, darifenacin MOA, indication, adverse effect?

• muscarinic antagonist (anticholinergic agent)

• atropine analogs; I: asthma, COPD; D: incontinence

• tachycardia, palpitations, urinary retention, urticaria

botulinum MOA, indication, adverse effect?

• blocks ACh exocytosis/release

• strabismus, overactive bladder, dystonia, hyperhidrosis, migraines, bruxism, wrinkles

• muscle weakness, loss of bladder control, hoarse voice, droop eyelids, vision change, dry mouth

cholinesterase inhibitors (cholinergic agents)? MOA, indication?

• pyridostigmine: MG + soman gas prophylaxis

• physostigmine: anticholinergic poison (atropine OD), glaucoma

• galantamine, donepezil: AD

cholinesterase inhibitors (cholinergic agents) adverse effects, drug interactions?

• pyridostigmine doesn’t cross BBB

• edrophonium helps Dx MG

• DUMBBELSS (defecation, urination, miosis, bronchorrhea, bronchospasm/bradycardia, emesis, lacrimation, salivation, sweating)

pralidoxime MOA, indication, adverse effect?

• cholinesterase regenerator

• Tx anticholinesterase poisoning (w/ atropine)

• neuromuscular weakness, respiratory arrest

function of alpha receptors? what do they bind?

• a1 → smooth muscle contraction

  • GPCR: Gq, IP3, DAG, PKC

• a2 → dec. sympathetic outflow

  • GPCR → Gi

function of beta receptors? what do they bind?

• B1 → inc. HR (1 heart)

  • GPCR → Gs, cAMP, AC

• B2 → broncho + vasodilates (2 lungs)

  • GPCR → Gs, cAMP, AC

phenylephrine MOA, indications, AE, CI?

• a1 agonist

• HTN, nasal congestion, septic shock, mydriasis

• AE: bradycardia, rebound rhinitis; CI: HTN, ventricular tachycardia

a2 agonists? indications? AE?

• clonidine → HTN, opioid dependence, ADHD

  • dizzy, dry mouth, constipation, sedation, rebound HTN/HTN crisis

• methyldopa → HTN during pregnancy

  • immunologic effects, Coombs + hemolytic anemia, autoimmune hepatitis

a antagonist? indications? AE

• terazosin (a1) → HTN, BPH (relax bladder, urethra/prostate smooth muscle)

  • dizzy, syncope + orthostatic hypotension

• phenoxybenzamine → HTN in pheochromocytoma (give b4 propranolol = prevent unopposed a-adrenergic stim.)

  • tachycardia, postural hypotension, congestion, inhibit ejaculation

B agonists? indications? AE, CI?

• dobutamine (B1) → cardio/septic/hypovolemic shock + HF

  • AE: HTN, tachycardia; CI: idiopathic hypertrophic subaortic stenosis

• albuterol (B2) → asthma

  • AE: tremors, nervousness, tachycardia, hypokalmia, HTN

B antagonist? indications? AE, CI?

• propranolol

• HTN, chest pain, cardio issues, migraines, pheochromocytoma (can masks hypoglycemia symptoms in diabetic pt.)

• AE: cardio issues, hypotension, sexual dysfxn, paresthesia, light-head; CI: cardiogenic shock, sinus bradycardia, asthma

norepinephrine MOA? indications? AE, CI?

• a + B agonist (no B2)

• HTN, shock (dopamine inhibits transport/reuptake of NE; reserpine dec. synth/storage of NE)

• AE: ischemic injury, tissue hypoxia, cardio issues, anxiety, headache; CI: hypovolemia

epinephrine MOA? indications? AE, CI?

• a + B agonist

• anaphylactic shock, cardiac arrest, v-fib, reduce bleeding during surgery, prolong local anesthetic

• AE: anxiety, headache, fear, palpitations, cardiac arrhythmias; CI: end-artery structures like fingers/toes

tyramine MOA? indications? AE, CI?

• release NE via MAO path

• narcolepsy + ADHD

• AE: tachycardia, HTN, tight chest, sweating, pallor; CI: antidepressant (inc. tyramine F = inc. NE → HTN + headache)

cocaine MOA? indications? AE? CI?

• reuptake inhibitor

• local anesthesia (blocks reuptake of NE → inc. NE in cleft)

• AE: tachycardia, HTN, dilated pupils, inc. body temp, resp. failure