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58 Cards in this Set

  • Front
  • Back
G protein Gs
(a) receptors
(b) Effector
(c) Second Messenger response
(a) beta1, beta2, D1, H2, V2
(b) Adenylyl cyclase
(c) increased cAMP
G protein Gi
(a) receptors
(b) effector
(c) second messenger response
(a) alpha2, M2, D2
(b) adenylyl cyclase
(c) decreased cAMP
G protein Gq
(a) receptors
(b) effector
(c) second messenger response
(a) alpha, M1, M3, H1,V1
(b) phospholipase
(c) increased IP3, increased IC Ca2+, DAG
Bethanechol
(a) classification
(b) clinical application
(c) action
(a) direct cholinergic agonist
(b) postop and neurogenic ileus and urinary retention
(c) activates bowel and bladder SM; resistant to AchE
Carbachol
(a) classification
(b) clinical application
(a) direct cholinergic agonist
(b) glaucoma, pupillary contraction, and release of intraocular pressure
Pilocarpine
(a) classification
(b) clinical application
(c) action
(a) direct cholinergic agonist
(b) potenti stimulator of sweat, tears, saliva
(c) contracts ciliary muscle of eye (open angle), pupillary sphincter (narrow angle); resistant to AChE
Methacholine
(a) classification
(b) clinical application
(c) action
(a) direct cholinergic agonist
(b) challenge test for diagnosis of asthma
(c) stimulates muscarinic receptors in airway when inhaled
Neostigmine
(a) classification
(b) clinical application
(c) action
(a) anticholinesterase
(b) postop and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular jct blockage (postop)
(c) increase endogenous Ach; no CNS penetration.
Pyridostigmine
(a) classification
(b) clinical application
(c) action
(a) anticholinesterase
(b) myasthenia gravis (long acting)
(c) increase enogenous Ach; increase strength; does not penetrate CNS
Edrophonium
(a) classification
(b) clinical application
(c) action
(a) anticholinesterase
(b) diagnosis of myasthenia gravis (extremely short acting)
(c) increase endogenous Ach
Physostigmine
(a) classification
(b) clinical application
(c) action
(a) anticholinesterase
(b) glaucoma (crosses BBB into CNS) and atropine overdose
(c) increase endogeous Ach
Echothiophate
(a) classification
(b) clinical application
(c) action
(a) anticholinesterase
(b) glaucoma
(c) increase endogenous Ach
Describe treatment for the following toxicity:
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, and Salivation (also abdominal cramp)
Cholinesterase inhibitor poisoning
Antidote: atropine (muscarinic antagonist) plus pralidoxine (chemical antagonist used to regenerate active cholinesterase).
Classification and Application of atropine in the eye
Muscarinig antagonist
Produce mydriasis and cycloplegia
Classification and Application of benzotropine
Muscarinig antagonist
Parkinson's disease
Classification and Application of Scopolopine
Muscarinig antagonist
Motion sickness
Classification and Application of oxybutynin, glycopyrrolate
Muscarinig antagonist
Reduce urgency in mild cystitis and reduce bladder spasms
Classification and Application of ipratropium
Muscarinig antagonist
Asthma, COPD
Classification and Application of Methscopolamine (also pirenzepine, propantheline)
Muscarinig antagonist
Peptic ulcer treatment
Atropine classification and effect
Muscularinic antagonist
Increase pupil dilation (cycloplegia)
Decrease airway secretions
Decrease stomach acid secretions
Decrease GI motility
Atropine toxicity
Increase body temperature, rapid pulse
Dry mouth
Flushed skin
Cycloplegia
Constipation
Disorientation
Can cause acute angle glaucoma in elderly, urinary retention in men with BPH, and hyperthermia in infants
Hexamethonium
(a) classification
(b) clinical use
(c) toxicity
(a) nicotinic antagonist
(b) ganglionic blocker. Used in lab models to prevent vagal reflex response to changes in BP (prevents reflex bradycardia by NE)
(c) severe orthostatic hypotension, blurred vision, constipation, sexual dysfct
Epinephrine
(a) classification
(b) mechanism/selectivity
(c) applications
(a)drug direct sympathomimetic
(b) alpha1,2 and beta 1,2 (low dose selective for beta 1)
(c) anaphylaxis, glaucoma (open angle), asthma, hypotension
Norepinephrine
(a) classification
(b) mechanism/selectivity
(c) applications
(a)drug direct sympathomimetic
(b) alpha1, alpha2>beta 1
(c) hypotension, (but decreased renal perfusion)
Isoprotenerenol
(a) classification
(b) mechanism/selectivity
(c) applications
(a) direct sympathomimetics
(b) beta1=beta2
(c) AV block (rare)
Dopamine
(a) classification
(b) mechanism/selectivity
(c) applications
(a) direct sympathomimetics
(b) D1=D2>beta>alpha, inotropic and chronotropic
(c) shock (increased renal perfusion), heart failure
Dobutamine
(a) classification
(b) mechanism/selectivity
(c) applications
(a) direct sympathomimetics
(b) beta1>beta2 inotropic but not chronotropic
(c) shock, heart failure, cardiac stress testing
Albuterol/Terbutaline
(a) classification
(b) mechanism/selectivity
(c) applications
(a) direct sympathomimetics
(b) alpha1>alpha2
(c) albuterol for acute asthma; terbulatine reduces premature uterine contractions
Ritodrine
(a) classification
(b) mechanism/selectivity
(c) applications
(a) direct sympathomimetics
(b) beta 2
(c) reduces premature uterine contractions
Amphetamine
(a) classification
(b) mechanism/selectivity
(c) applications
(a) indirect sypmathomimetics
(b) indirect general agonist, released stored catecholamines
(c) narcolepsy, obesity, ADD
Ephedrine
(a) classification
(b) mechanism/selectivity
(c) applications
(a) indirect sympathomimetics
(b) indirect general agonist, releases stored catecholamines
(c) nasal decongestion, urinary incontinence, hypotension
Cocaine
(a) classification
(b) mechanism/selectivity
(c) applications
(a) indirect sympathomimetics
(b) indirect general agonist, uptake inhibitor
(c) causes vasoconstriction and local anesthesia
Clonidine, alpha methyldopa
(a) classification
(b) mechanism/selectivity
(c) applications
(a) sympathoplegics
(b) centrally acting alpha 2 agonist, decreased central adrenergic outflow
(c) HTN, esp w/renal disease (no decr in blood flow to kidney)
Phenoxybenzamine
(a) classification
(b) applications
(c) toxicity
(a) non selective alpha blocker
(b) pheochromocytoma (use phenoxybenzamine before removing tumor since high levels of released catecholamines will not be able to overcome blockage)
(c) orthostatic hypotension, reflex tachycardia
Alpha 1 selective blockers
Prazosin, terazosin, doxazosin
Prazosin, terazosin, doxazosin
(a) classification
(b) applications
(c) toxicity
(a) alpha 1 selective blocker
(b) HTN, urinary retention in BPH
(c) 1st dose orthostatic hypotension, dizziness, headache
Mirtazapine
(a) classification
(b) application
(c) toxicity
(a) alpha 2 selective blocker
(b) depression
(c) sedation, increased serum cholesterol, increased appetite
Beta blocker: clinical applications
HTN (decr CO and renin)
Angina pectoris (decrease HR, contractility, resulting in decr O2 consumption)
MI (beta blockers decrease mortality)
SVT-propranolol, esmolol (decr AV conduction velocity)
CHF (slows prgoression of chronic failure)
Glaucoma-timolol-decreases secretion of aqueous humor
Nonselective antagonists
Propranolol, timolol, nadolol, pindolol, and labetalol
Beta 1 selective antagonists
Acebutolol (partial agonist), betaxolol, esmolol (short acting), atenolol, metoprolol
Non selective alpha and beta antagonists
Carvediolol, labetalol
Partial beta agonists
Pindolol, acebutolol
Toxicity of beta blockers
Impotence, exacerbation of asthma, CV adverse effects (bradycardia, AV block, CHF), CNS adverse effects (sedation, sleep alterations); use with caution in diabetics.
Synthesis of histamine
Histidine converted to histamine by histadine decarboxylase
Location of histamine
Circulating basophils and mast cells
H1 antagonists
(a) list common
(b) clinical use
(c) sedation, dry mucosa
(a) diphenydramine, promethazine, chlorpheniramine, hydroxyzine, fexofenadine*, loratadine*, cetirizine *
*indicates no CNS entry
(b) allergic rxns, motion sickness, OTC (sleep aids and cold meds)
(c) sedation, dry mucosa
H2 antagonists
(a) list common
(b) clinical use
(c) notes/toxicity
(a) cimetidine, ranitidine, famotidine, nizatidine
(b) peptic ulcer disease, GERD, zollinger ellison syndrome
(c) cimetidine: P450 inhibition, antiandrogen effect
Synthesis and degradation of serotonin
Tryptophan converted to 5HT by tryptophan hydroxylase. MAO degrades serotonin into 5H1AA
5HT1 (A-F)
(a) second messenger
(b) action
(a) Gi, decr cAMP
(b) CNS, behavioral effects (sleep, feeding, thermoreg, anxiety), vasoconstriction
5HT2(A-C)
(a) second messenger
(b) action
(a) Gq; increase IP3, DAG
(b) CNS, behavioral effects, smooth muscle contraction, platelet aggregation
5HT3
(a)second messenger
(b) action
(a) ion channel
(b) CNS (area postrema), PNS, emesis, anxiety
5HT4
(a) second messenger
(b) action
(a) Gs; increase cAMP
(b) CNS: neuronal excitation, GI motility
Sumatriptan, naratriptan
(a) mechanism of action
(b) clinical use
(c) notes/toxicity
(a) 5HT1D agonist
(b) migraines
(c) n/a
Buspirone
(a) mechanism of action
(b) clinical use
(c) notes/toxicity
(a) 5HT1A partial agonist
(b) anxiety disorders
(c) lower addition potential than other drugs like benzos
Ondasetron
(a) mechanism of action
(b) clinical use
(c) notes/toxicity
(a) 5HT3 antagonist
(b) emesis
(c) mainly for postop or chemo induced n/v
SSRI's
(a) mechanism
(b) clinical use
(c) notes/toxicity
(a) selectively block 5HT reuptake
(b) anxiety disorders, depression
(c) sexual dysfct, interaction w/MAOI's can lead to serotonin syndrome
Ergot alkyloids (ergonovine, ergotamine, methysergide, bromocriptin, pergolide, LSD)
(a) mechanism of action
(b) clinical use
(c) notes/toxicity
(a) agonists, partial agonists, and antagonists at 5HT and alpha receptors; some are agonists or partial agonists at DA receptors
(b) postpartum hemorrhage (ergonavine, ergotamine)
-migraines (ergotamine for acute, methysergide for prophylaxis)
-parkinson's disease, hyperprolactinemia (bromo, pergolide)
-abuse (LSD)
(c) Ergotism (St. Anthony's fire)
-mental disorientation, convulsions, muscle cramps, hallucinations, dry gangrene of extremities
MAOI's
(a) mechanism of action
(b) clinical use
(c) notes/tox
(a) inhibit metabolism of 5HT, NE, and DA by MAO
(b) depression
(c) non selective MAO inhibitors
-tyramine ingestions can lead to hypertensive crisis