Pharm 1 (autonomics, hematologics, antineoplastics) Flashcards
Ephedrine
Indirect sympathomimetic - indirect general agonist, releases stored catecholamines
Nasal decongestion, urinary incontinence, hypotension
pseudoephedrine commonly used
*activity reduced by prior tx w/ reserpine/guanethidine
Amphetamine
Indirect sympathomimetic - indiret general agonist, reuptake inhibitor, & releases stored catecholamines
Tx - Narcolepsy, obesity, attention deficit disorder
*activity abolishied by prior tx w/ reserpine/guanethidine
Cocaine
Indirect symphathomimetic - indirect general agonist & reuptake inhibitor
Causes vasoconstricion & local anesthesia
NEVER give β-blockers if cocaine intoxication is suspected (can lead to unopposed α1 activation & extreme hypertension)
Prazosin
Terazosin
Doxazosin
Tamsulosin
α1 selective antagonist (-osin)
Urinary symptoms of BPH, HTN, PTSD (prazosin)
Tamsulosin - solely used for BPH (α1a selective)
AE - 1st dose orthostatic HoTN, dizziness, headache
Yohimbine
α2 antagonist - increases central sympathetic activity
= ↑ BP & HR
Tx - male erectile dysfunction, HoTN
AE - anxiety, (excess pressor effect if NET1 is blocked)
Phenoxybenzamine
Irreversible nonselective α antagonist (long DoA)
= ↓ BP, ↑ HR (baroreflex +)
Tx - pheochromocytoma (catecholamine releasing tumor in the adrenal gland)
AE - orthostatic HoTN, reflex tachycardia, MI
Phentolamine
Reversible nonselective α antagonist
Given to Pt on MAOI who eat tyramine-containing foods
Mirtazapine
α2 selective antagonist
Tx - Depression
AE - Sedation, ↑ serum cholesterol & appetite
Labetalol
Carvedilol
Nonselective α- & β-antagonists
=↓ BP w/ limited HR ↑ (↓ reflex tach by also blocking α1)
Tx - HTN
(-ilol & -alol instead of -olol of B selective)
Nadolol
Pindolol
Propranolol
Timolol
Nonselective β-antagonists (β1=β2)
= ↓ HR, BP & reduce Renin
Tx - HTN, angina pectoris, arrhytmias, migraine, hyperthyroidism
↑ bronchospasm (β2)
Atenolol Metoprolol Esmolol Beliprolol Acebutolol
Selective β-antagonists (β1>β2)
= ↓HR, BP & reduce renin
safer on asthma
Tx - HTN, angina pectoris, arrhytmias
Pindolol & Acebutolol
β-antagonists w/ ISA (intrinsic sympathomimetic activity)
=↓BP, but only modestly ↓ HR
block receptors but elicit a small response
Tx - HTN, arrhytmias, migraine
may avoid worsening of bradycardia
β-blockers
-olol (-alol, -ilol)
Tx - angina pectoris (↓HR & contractility = ↓ O2 need)
- MI (↓ mortality - metoprolol, carvedilol, bisoprolol)
- SVT (↓ AV conduction, class II - metoprolol esmolol)
- HTN (↓ CO, ↓ renin (due to blockade of JGA cells)
- CHF (slows progression of chronic failure)
- Glaucoma (↓ secretion of aqueous humor - timolol)
AE - impotence, CV (bradycardia, AV block, CHF), dyslipidemia (metoprolol), CNS (seizures, sedation)
may cause exaceration in asthma/COPD (especially nonselective, through blockade of β2)
Phenylephrine
Direct sympathomimetics - α1>α2 (=vasoconstriction)
= ↑ BP, ↑ TPR & reflex bradycardia
Tx - HoTN, ocular procedures (mydriatic), decongestant
Albuterol Salmeterol Terbutaline (Metaproterenol) (Ritodrine)
Direct sympathomimetics - β2>β1 (=bronchorelaxation)
Tx - Acute asthma (albuterol)
- Long-term asthma/COPD (Salmeterol) - Reduce premature uterine contractions (terbutaline) - ritodrine designed specifically as uterine relaxant
Isoproterenol
Direct sympathomimetic - β1=β2
= ↓ TPR, ↑ HR, ↑ myocardial contractility
Tx - Electrophysiologic evaluation of tachyarrhythmias
can worsen ischemia
Dobutamine
Direct Sympathomimetic - β1>β2,
= + inotropic, + chronotropic, (TPR not affected)
Tx - heart failure (inotropic>chronotropic), stress testing
Epinephrine
Direct sympathomimetic = β>α
(α effects dominate at high doses)
Tx - Anaphylaxis, open angle glaucoma, asthma, HoTN
CI - PT using nonselective β-blockers (=severe vasoconstriction)
Norepinephrine
Direct sympathomimetic = α1>α2>β1
↑ BP, PP, TPR & Coronary flow, ↓ CO & renal perfusion
Tx = HoTN (but ↓ renal perfusion) - dose titration needed
Dopamine
Direct sympathomimetic - D1=D2>β>α
(inotropic & chronotropic α effects predominate at high dose)
Unstable bradycardia, heart failure, shock
Hypovolemia should always be corrected before use
Avoid w/ MAOI or tricyclic antidepressants
Fenoldopam
Direct agonist - D1 selective
Tx - Hypertensive crisis (renal, mesenteric, peripheral & coronary vasodilation) (= renal blood flow maintained & natriuresis promoted)
AE - HoTN
Clonidine
α-methyldopa
Sympatholytics - α2 selective agonist
(↓ BP by ↓ central sympathetic outflow)
Tx - Hypertensive urgency (doesn’t ↓ renal blood flow)
α-methyldopa for HTN in pregnancy (safe in pregnancy but causes DIrect Coombs + hemolytic anemia, SLE-like syndrome)
Clonidine AE - CNS depression bradycardia, HoTN, respiratory depression & small pupil size
Atropine
Homatropine
Tropicamide
Muscarinic antagonists
Organ system - eye
Tx - produce mydriasis & cycloplegia
Ipratropium
tiotropium
Muscarinic Antagonists
Organ system - respiratory
Tx - COPD, asthma (↓ bronchoconstriction & bronchial secretions)
Atropine
Muscarinic antagonist - used to treat bradycardia & for ophthalmic applications
Blocks DUMBBeLSS
Eye - pupil dilation, cycloplegia airway- ↓ sectretions Stomach - ↓ acid secretion Gut - ↓ motility bladder - ↓ urgency in cystitis
AE - Hot, Dry, Red, Blind, Mad
↑ temp (by ↓ sweating); rapid pulse; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation
Causes acute angle-closer glaucoma in elderly (due to mydriasis), urinary retention in men w/ prostatic hyperplasia, & hyperthermia in infants
Benztropine
Muscarinic antagonist
Organ system - CNS
Tx - Parkinson disease
=re-establishes dopaminergic-cholinergic balance
Scopolamine
Muscarinic antagonist
Organ system - CNS
Tx - Motion sickness
Oxybutynin
Darifenacin
Solifenacin
muscarinic antagonist
Organ system - Genitourinary
Tx - Reduce urgency in mild cystitis & ↓ bladder spasms
(Other agents - tolterodine, fesoterodine, trospium)
Hexamethonium
Mecamylamine
Nicotinic Antagonists
↓ predominant autonomic tone & prevent baroreflex
SANS - arterioles = vasodialtion & HoTN
- Veins = Dilation, ↓ venous return, ↓ CO
- Sweat glands = Anhidrosis
PANS - Heart = tachycardia
- Iris = Mydriasis
- Ciliary muscle = Cycloplegia (loss of accommodation)
- GI = ↓ tone & motility = constipation
- Bladder = urinary retention
- Salivary glands = Xerostomia
Succinylcholine
d-Tubocurarine
Nicotinic Antagonists
block Nm channel (neuromuscular blockade)
S-bind & keep channel open=persistent depol & paralysis
T-bind and prevent openeing of channel
Tx of convulsions, & ↓ neuromuscular transmission during anesthesia; used in tracheal intubation to control ventilation
Methacholine
Cholinomimetic agent - Direct agonist
= stimulates muscarinic receptors in airway when inhaled
Tx - Challenge test for diagnosis of asthma
Carbachol
Cholinomimetic agent - Direct agonist
= “CARBon copy” of AcetylCHOLamine
Tx = Glaucoma, pupillary constriction, & relief of intraocular pressure
High doses may induce cardiac arrest
Bethanechol
Cholinomimetic agent - Direct agonist
= activates Bowel & Bladder smooth muscle cells
- resistant to AChE
Tx - Post-op ileus, neurogenic ileas, urinary retention