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Adrenergic and Cholinergic
Sympathetic and Cholinergic drugs
60
Pharmacology
Professional
01/25/2010

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Cards

Term
Epinephrine
Definition
-all alpha and Beta receptors
-used to prevent anaphylaxis
-vasoconstriction for local anasthetics
Term
Cocaine
Definition
-Uptake1 inhibitor (keeps NE in post-synaptic jxn)
- ^BP and ^HR
-Local anasthetic, prevents bleeding
Term
Tyramine
Definition
-"Wine and Cheese" (w/ MAO inhibitor)
-Strong indirect sympathomimetic
- Get hypertensive crisis
Term
Metyrosine
Definition
-Tyrosine Hydroxylase competitive inhibitor
-Stops catecholamine production
Tx: phaeochromocytoma
Sdx: depression, crystalluria, upset GI
Term
Methyldopa
Definition
-"False Transmitter"
-Acts in CNS to depress sympathetics
Tx: HTN
Term
Guanethidine
Definition
-Prevents post-synaptic release of NE from (catecholamine inhibitor)
Term
Reserpine
Definition
-Blocks VMAT, keeps NE in cytosol longer(broken down by MAO and COMT)
Tx: HTN
DO NOT USE with Hx of depression
Term
Phentolamine
Definition
-Blocks alpha receptors (Epi reversal)
Term
Norepinephrine
Definition
alpha 1,2 and Beta 1 agonist (not Beta 2)
Term
Isoproterenol
Definition
Beta 1 & 2
Term
Ephedrine(pseudophedrine)
Definition
-Most activity through indirect sympathomimetics
-orally active (MAO and COMT resistant)
-some direct action at Beta receptors
Tx: Decongestant (vasoconstriction)
Sdx: ^BP (stroke), Cardiac arrhythmias, CNS stimulation and seizure
Term
Ephedrine + MAO inhibitor
Definition
Potentiation
Term
Phenylephrine
Definition
-alpha 1 receptor agonist (vasoconstrict)
- Indirect action: used to treat Atrial tachycardia by ^ BP and ^ vagal tone, lowering HR
Term
Clonidine
Definition
-alpha 2 receptor agonist (centrally acting: Brainstem)
-Decrease symp activity @ heart and blood vessels
Tx: Centrally acting anti-hypertensive
Sdx: dry mouth, sedation
Term
Albuterol
Definition
-Beta2 receptor agonist (selective)
-Rescue inhaler
*not broken down by MAO
Term
Salmeterol
Definition
-Long acting Beta2 receptor agonist
*not a rescue inhaler
Term
Dopamine
Definition
-D1 receptor agonist (^ blood flow to kidneys
-Some direct alpha and beta receptor agonist w/ indirect sympathomimetic
Tx: Shock (IV infusion)
Keeps periph BP ^ while keeping kidneys perfused
Term
Phentolamine
Definition
-Non-selective competitive alpha antagonist (alpha blocker)
*binds reversibly
Term
Effects of alpha receptor antagonism
Definition
-decreased BP
- ^HR
-Nasal congestion (vasodilation)
-decreased ability to ejaculate
-Sedation/depression (CNS)
Term
Ritodrine
Definition
-B2 selective agonist (systemic)
Tx: premature uterine contractions
Term
Dobutamine
Definition
-Beta1 agonist (also B2 and A1)
-^ chronotropics of heart (^contractility)
Tx: acute heart failure, "stress test"
*must be IV
Term
Phenoxybenzamine
Definition
- Non-selective alpha blocker (irreversible)
*has spare receptors
Tx: Phaeochromocytoma
**NOT useful in Tx of HTN because blocks alpha 2 receptors causing blockage of NE feedback loop (^BP)
Term
Prazosin (Terazosin)
Definition
-Selective Alpha1 antagonist (decrease TPR and decrease smooth muscle stimulation)
Tx: HTN, CHF, and BPH
**First dose phenomenon (hypotension and/or syncope)
Term
Indications for Beta Blockers
Definition
-Angina
-Cardiac Arrhythmia
-HTN (dont work in normotensive ind)
-Post MI
-CHF
Term
Propranolol
Definition
-Competitive Beta 1 & 2 antagonist
Tx: HTN, Angina, Ischemic Heart Disease
**Rapidly degraded by the liver (short half-life)
Sdx: Cardiac Depression, Contraindicated for Asthmatic (blocks B2 receptors), Diabetics cant tell when tachycardic (dont know when hypoglycemic)
Term
How do Beta Blockers treat HTN
Definition
Initial and sustained decrease in Cardiac output w/ initial compensatory ^ in BP. Periph resistance falls slowly resulting in decreased BP
*B-receptors in vasculature are not normally activated
Term
Metoprolol
Definition
-Cardioselective B-blocker (B1)
-Good for asthmatics
-Short half-life... some pharmacodynamic problems (slow hydroxylators) can have ^ blood levels
Term
Atenelol
Definition
-Once daily cardioselective B-blocker
-different clearance mechanism (renal)
Term
Pindolol
Definition
-Partial agonist @ all Beta receptors
(Intrinsic Sympathomimetic Activity)
**less cardiac depression, less tendency for bronchoconstriction), reduces periph resistance
Term
Esmolol
Definition
-Super short acting beta blocker
Tx: surgery to protect heart from catecholamines
broken down rapidly
Term
Nicotinic (Ach) receptors
Definition
-ligand gated
-two types Ng and Nn (ganglionic)
-Nm (Neuromuscular jxn)
Term
Muscarinic
Definition
-Cardiac (decrease)
-Glands (increase)
Term
Pilocarpine
Definition
-Muscarinic agonist (salivating, sweating)
Tx: Open angle glaucoma, Sjogren's/Cancer radiotherapy(dry mouth)
Term
Metacholine
Definition
-Synthetic Ach analog (muscarinic agonist)
-used to dx Asthma as provocative test
**DO not use w/ peptic ulcer, coronary insufficiency or known asthma
***Never IV or IM causes cardiac arrest and acute resp distress
Term
Bethanochol
Definition
Term
Bethanachol
Definition
-Ach agonist
-Poorly absorbed in the gut and reabsorbed in kidney (so it stays there)
Tx: To stimulate GI (post-surgery) and Urinary retention
Term
Atropine
Definition
-Muscarinic Antagonist
Term
Atropine Effects
Definition
-decreased glandular secretions (dry mouth/ hyperthermia in kids)
- Pupil dilatation (glaucoma exacebation)
- ^ HR
- Blocks vagal bronchoconstriction
-Decrease bladder tone and ^ sphincter tone (retention)
-decrease GI motility (constipation)
-anti-parkinsons and motion sickness
Term
Scopolamine
Definition
-Muscarinic Antagonist (highly lipophilic) *gets into CNS
- Patch for motion sickness
Sdx: Dry mouth, blurred vision
Term
Ipratropium
Definition
-Muscarinic antagonist w/ (+) charge (won't cross biomembranes)
Tx: COPD and Asthma
*Used with albuterol for additive effects
Term
Tolteridine
Definition
-Non-specifice muscarinic antagonist
Tx: Overactive Bladder
Term
Nicotine
Definition
-Agonist @ nicotinic receptors
- Autonomic ganglia and NM jxn
Term
Acute Nicotine Toxicity (blockade)
Definition
Ach binds and is rapidly degraded in post-synaptic jxn. Nicotine binds and does not leave rapidly so receptor can't repolarize causing "block"
- ^ Sympathetic Cardiovascular
Term
Varenicline
Definition
-Partial Nicotinic agonist (anti-tobacco)
-Mimics nicotine @ "reward center" & reduces withdrawal
-Don't get 'rewarded' for cig
Sdx: Borderline psychoses?
Term
Hexamethonium
Definition
-Ach antagonist @ ganglionic nicotinic receptors
- paralyzes entire Autonomic Nervous sys
Tx: HTN, dissecting AA, autonomic hyperreflexia, control hemorrhage in surgery
**Blocks predominant autonomic tone
Term
Hexamethonium Effects (arterioles)
Definition
Vasodilation (hypotension)
Term
Hexamethonium Effects (sweat glands)
Definition
decreased perspiration
Term
Hexamethonium effects (heart rate)
Definition
Tachycardia
Term
Hexamethonium (Eye)
Definition
Pupil dilation (mydriasis)
blurred vision (cyclopegia)
Term
Hexamethonium (gut)
Definition
Constipation
Term
Hexamethonium (Bladder)
Definition
Urinary Retention
Term
Hexamethonium (Salivary glands)
Definition
Dry mouth
Term
Edrophonium
Definition
Reversible cholinesterase inhibitor (short half life)
-Used to test for Myasthenia Gravis
Term
Physostigmine
Definition
-Cholinesterase 'substrate inhibitor'
-serves as a substrate that forms a more stable bond with cholinesterase, takes longer to be hydrolyzed
Term
Echothiophate
Definition
-Cholinesterase inhibitor
-Forms permanent bond w/ enzyme (phosphorylation)
Term
Tx uses of cholinesterase inhibitors
Definition
- ^ GI motility or bladder atony
- glaucoma
- Alzheimers??
- Myasthenia gravis
**can cause depolarizing blockade in normal individuals
Term
Neostigmine
Definition
-Cholinesterase inhibitor
-Marked GI effect because not well absorbed in gut, low bioavailability
Term
Effects of Organophosphate Cholinesterase inhibitor (nicotinic)
Definition
-Depolarizing blockade a NM jxn
muscle weakness> resp failure > death
Term
Effects of Organophosphate Cholinesterase inhibitor (muscarinic)
Definition
-hyperactive periph Parasymps
bradycardia>arrest
-hyperactive CNS
decrease resp drive and seizures/convulsions
Term
Dumbells (Nerve gas poisoning)
Definition
D-diarrhea
U-Urination
M-Miosis
B-Bronchospasm and Bradycardia
E-Emesis
L-Lacrimation
S-Salivation
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