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137 Cards in this Set
- Front
- Back
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Cholinergic Nicotinic DIRECT Agonists
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ACh, Carbachol, Nicotine
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Cholinergic Nicotinic/Muscarinic INDIRECT REVERSIBLE Agonists
(Competitive Inhibitors of Cholinesterase -Rapidly Reversible) |
Tacrine, Edrophonium, Donepezil, Galantamine
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Cholinergic Nicotinic/Muscarinic INDIRECT REVERSIBLE Agonists
(Carbamate Inhibitors - Long Lasting) |
PHYSOSTIGMINE, RIVASTIGMINE, Neostigmine, Physostigmine
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Cholinergic Nicotinic/Muscarinic INDIRECT IRREVERSIBLE Agonists
(Cholinesterase Inhibitors - Organophosphates highly soluble) |
Echothiophate, Parathion, DFP
Tabun, Sarin, Soman, VX (nerve gases) Reactivation of enzyme by Pralidoxime and 2-PAM |
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Cholinergic Nicotinic NON-DEPOLARIZING NON-COMPETITIVE Antagonists
Nn (Ganglionic Block) |
Hexamethonium
(not clinically used) |
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Cholinergic Nicotinic NON-DEPOLARIZING COMPETITIVE Antagonists
Nn (Ganglionic Block) |
Trimethapan, Mecamylamine
(not clinically used) |
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Cholinergic Nicotinic DEPOLARIZING Antagonists
Nn (Ganglionic Block) |
Nicotine, Varenicline (partial agonist)
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Cholinergic Nicotinic NON-DEPOLARIZING Antagonists
Nm Neuromuscular (Competitive) |
pancuronium, vecuronium, rapacuronium, rocuronium, cisatracurium, atracurium, mivacurium
d-Tubocurare (some Nn blockade and release of histamine) |
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Cholinergic Nicotinic DEPOLARIZING Antagonists
Nm Neruomuscular |
Succinylcholine (short acting), Nicotine
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Cholinergic Nicotinic Antagonists
CONTRAINDICATIONS Nm Neuromuscular |
Prolonged apenea ppl w/o pseudocholinesterase so there is excess succinylcholine
Electrolyte imbalance b/c excess K release Malignant Hyperthermia (genetic predisposition; succinlycholine w/chlorinated hydrocarbon) |
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Cholinergic Muscarinic DIRECT Agonists
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Ach, Methacholine, Carbacol, Bethanechol, Pilocarpine, Muscarine
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Cholinergic Muscarinic Antagonists
(Natural Belladonna Aalkaloids) |
Scopolamine (motion sickness)
Atropine (OP poisoning) |
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Cholinergic Muscarinic Antagonists
(Synthetics - Asthma and COPD) |
Ipratropium (contraindicated w/soy allergy)
Tiotropium |
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Cholinergic Muscarinic Antagonists
(Synthetics - Parkinsons) |
Benzotropine
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Cholinergic Muscarinic Antagonists
(Synthetics - Overactive Bladder M3) |
Tolteridine, Oxybutynin, Trospium
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Cholinergic Muscarinic Antagonists
(Synthetics - IBS) |
Dicyclomine, Propantheline
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Cholinergic Muscarinic Antagonists
(Synthetics - Gastric Acid Secretion M1) |
Pirenzipine, Telenzipine
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Cholinergic Muscarinic Antagonists
(Synthetics - Antitussive) |
Homatropine
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Cholinergic Muscarinic Antagonists
(Synthetics - Opthalmological - Mydriasis and cycloplegia) |
Cyclopentolate, Tropicamide
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Cholinergic Muscarinic Antagonists
(Contraindications) |
Open Angle Glaucoma
Increased IOP narrow-angle glaucoma Treatment: Pilocarpine |
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Cholinergic Muscarinic Antagonists
(Poisonings) |
Jimson Weed, Atropine, Scopolamine, H1 (Histamine Antagonists), Phenothiazines, Tricyclic Antidepressants (Protriptyline & Olanzipine)
Dry as a bone, Mad as a hatter, Red as a beet, Blind as a bat |
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Adrenergic Receptors α1
(Type and Drug Affinity) |
Gq (squeeze)
1. NE 2. Epi postsynaptic (stimulatory) |
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Adrenergic Receptors α2
(Type and Drug Affinity) |
Gi (inhibitory)
1. Epi 2. NE presynaptic / postsynaptic |
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Adrenergic Receptors β1
(Type and Drug Affinity) |
Gs (stimulatory)
1. Epi = NE postsynaptic |
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Adrenergic Receptors β2
(Type and Drug Affinity) |
Gs then Gi (Gi only after Gs has been activated - method of self-regulation)
1. Epi >> NE presynaptic / postsynaptic |
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Adrenergic Receptors β3
(Type and Drug Affinity) |
Gs & Gi
1. NE 2. Epi postsynaptic (mostly on bladder) |
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Adrenergic DIRECT NON-SELECTIVE Agonists
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Epinephrine (α1,2 β1-3)
NE (α1,2 β1,3) Oxymetazoline (α1,2) Isoproterenol (β1-3) |
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Adrenergic DIRECT SELECTIVE Agonists
(α's) |
Phenylephrine & Desglymidodrine (α1)
Clonidine, Apraclonidine, Brimonidine, α-methyl-NE, Guanfacine, Guanabenz (α2) |
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Adrenergic DIRECT SELECTIVE Agonists
(β's) |
Dobutamine (β1) - (also is α1 moderate)
Albuterol, Terbutaline (β2) (short-acting) Salmeterol, Formoterol (β2) (long-acting) |
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Adrenergic MIXED Agonists
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Ephedrine
Mephentermine (α1 & releasing agent) |
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Adrenergic RELEASING AGENT INDIRECT Agonists
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Amphetamine
Tyramine (Tyrosine break down product) Methamphetamine |
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Adrenergic UPTAKE INHIBITOR INDIRECT Agonists
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Cocaine (NE & Dopamine transporters)
Desipramine, Isocyanines, Methamphetamine |
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Adrenergic MAO/COMT INHIBITOR INDIRECT Agonists
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Pargyline, Entacapone, Methamphetamine
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Adrenergic Miscellaneous INDIRECT Agonist
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Forskolin, Milrinone
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Adrenergic NON-SELECTIVE α ANTAGONISTS
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Phentolamine
Phenoxybenzamine (irreversible; mod α2) |
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Adrenergic SELECTIVE α1 ANTAGONISTS
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Prozasin, Doxazosin, Terazosin, Alfuzosin
Talmsulosin, Silodosin (α1a for prostate) Carvediol, Labetalol (β blockers as well) |
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Adrenergic SELECTIVE α2 ANTAGONISTS
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Yohimbine, Idozoxan (no real clinical use)
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Adrenergic SELECTIVE β1 ANTAGONISTS
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Metoprolol, Atenolol, Bisoprolol, Esmolol, Nebivolol
Labetalol, Carvedilol (α1 antagonists as well) |
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Adrenergic SELECTIVE β1 & β2 ANTAGONISTS
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Propanolol, Pindolol, Timolol
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Adrenergic SELECTIVE β3 ANTAGONISTS
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Nebivolol, Pindolol (partial agonists)
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Epinephrine
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PHARMACOLOGIC EFFECT: Bronchodialation (β2), Vasoconstriction (α1,α2), Cardiac Stimulation (β1), Mydrasis (α1)
CLINICAL USE: Hypersensitivity Rxn, Cardiac Arrest, Hemostatic Agent, Local Anesthetics, Mydrasis for surgery |
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Norepinephrine
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PHARMACOLIGIC EFFECT:
Vasoconstriction (α1,α2), Very little cardiac stimulation as vagal "muscarinic" reflex will win the battle CLINICAL USE: Low Blood Pressure |
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Dopamine
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PHARMACOLOGIC EFFECT: Renal Vasodialation (D1), Vasoconstriction (α1), Cardiac Stimulation (β1)
CLINICAL USE: Cardiogenic and Septic Shock, Severe Congestive Heart Failure |
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Oxymetazoline
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PHARMACOLOGIC EFFECT:
Vasoconstriction (α1) CLINICAL USE: Nasal Congestion, Allergic Conjunctivitis SIDE EFFECTS: Rebound Congestion |
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Phenylephrine
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PHARMACOLOGIC EFFECT: Vasoconstriction (α1), Mydrasis (α1)
CLINICAL USE: Nasal Congestion, Ocular Surgery SIDE EFFECTS: Can precipitate angle closure glaucoma, taken orally: hypertension |
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Desglymidodrine
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PHARMACOLOGIC EFFECT:
Vasoconstriction (α1) CLINICAL USE: Hypotension due to Autonomic Neuropathy, Severe Orthostatic Hypotension SIDE EFFECTS/DRUG INTERACTIONS: Supine Hypertension, Reflex Bradycardia, Cardiac Glycosides, |
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Clonidine
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PHARAMACOLOGIC EFFECT:
Decrease Sympathetic Drive, Increase Parasympathetic Outlfow, Decrease NE Release, Vasoconstriction, Sedation, Analgesia (α2) CLINCAL USE: Hypertension, Adjunctive Alleviation of Sever Pain, Adjunctive use in Anesthesia SIDE EFFECTS: Drowsiness, Dry Mouth, Sexual Dysfunction, Bradycardia, Embryotoxic |
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α-methyl-dopa
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PHARMACOLOGIC EFFECT: Decrease Sympathetic Drive, Increase Parasympathetic Outlfow, Decrease NE Release, Vasoconstriction, Sedation (α2)
CLINICAL USE: Pregnancy-induced hypertension |
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Apraclonidine & Brimonidine
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PHARMACOLOGIC EFFECT: Reduction of aqueous humor (α2)
CLINICAL USE: Reduction of Intraocular Pressure |
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Isoproterenol
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PHARAMACOLOGIC EFFECT: Cardiac Stimulation (β1), Bronchodialation (β2), Vasodialation (β2,3), GI Relaxation (β2), Bladder Relaxation (β3)
CLINICAL USE: Cardiac Resuscitation COMT Substrate, Poor MAO substrate |
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Dobutamine
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PHARMACOLOGIC EFFECT: Cardiac Stimulation (β1), Vasoconstriction (α1)
CLINICAL USE: Heart Failure COMT & MAO substrate |
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Albuterol/Terbutaline
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PHARMACOLOGIC EFFECT: Bronchodialation (β2), Chronotropic Effect (β1,2)
CLINICAL USE: Asthma (short-term) SIDE EFFECTS: Tremors, Restlessness, (Hypotension, tachycardia, angina), (Hyperglycemia, hyperlipidemia), Decreases [K] |
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Salmeterol/Formeterol
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PHARMACOLOGIC EFFECTS: Bronchodialation (β2), Chronotropic Effect (β1,2)
CLINICAL USE: Adjunctive Treatment for Asthma (prophylactic treatment) SIDE EFFECTS: Tremors, Restlessness, (Hypotension, tachycardia, angina), (Hyperglycemia, hyperlipidemia), Decreases [K] Formeterol can cause Astma related death. |
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Phenoxybenzamine
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PHARMACOLOGIC EFFECT: Hypotension (α1), Chronotropic Effect (α1,2)
CLINICAL USE: Operable Pheochromocytoma, Adjunctive Treatment in Inoperable Pheochromocytoma SIDE EFFECTS: Nasal Stuffiness, Hypotension, tachycardia, myocardial infarction, mutagenic IRREVERSIBLE |
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Phentolamine
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PHARMACOLOGIC EFFECT: Vasodialation of arteries (α1), Reflex Tachycardia (α1,2)
CLINICAL USE: Preoperative in Pheochromocytoma, Prevention of extravasation-induced necrosis SIDE EFFECTS: Nasal Stuffiness, Hypotension, Tachycardia |
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Prazosin
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PHARMACOLOGIC EFFECTS: Vasodilation of arteries and veins, Relaxation of Smooth Muscle, Depression baroreflex (α1), Non-selective phosphodiesterase (PDE) inhibitor, Anitproliferative & Antiapoptic (quinazoline effects)
CLINICAL USE: Alternative treatment of hypertension SIDE EFFECTS/DRUG INTERACTIONS: Strong 1st dose effect, Dizziness, Syncope, Nasal Stuffiness, Hypotension, Tachycardia, VIAGRA |
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Terazosin/Dozazosin
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PHARMACOLOGIC EFFECTS: Vasodilation of arteries and veins, Relaxation of Smooth Muscle, Depression Baroreflex (α1), Apoptosis of Smooth Muscle
CLINICAL USE: Alternative treatment of hypertension, Benign Prostate Hyperplasia SIDE EFFECTS: Strong 1st dose effect, Dizziness, Syncope, Nasal Stuffiness, Hypotension, Tachycardia |
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Alfuzosin
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PHARMACOLOGIC EFFECTS: Vasodilation of arteries and veins, Relaxation of Smooth Muscle, Depression Baroreflex (α1), Apoptosis of Smooth Muscle
CLINICAL USE: Benign Prostate Hyperplasia SIDE EFFECTS/DRUG INTERACTIONS: Lesser 1st Dose Effect, Dizziness, Nasal Stuffiness, Hypotension, Tachycardia, ERYTHOMYCIN & KETOCONAZOLE Metabolized by CYP3A4 |
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Tamsulosin/Silodosin
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PHARMACOLOGIC EFFECT: Relaxation of Prostate and Smooth Muscle (α1a)
CLINICAL USE: Benign Prostate Hyperplasia SIDE EFFECTS/DRUG INTERACTIONS: Lesser 1st dose effect, Nasal Stuffiness, Hypotension, Tachycardia, ERYTHOMYCIN & KETOCONAZOLE Metabolized by CYP3A4 |
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Propanolol
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PHARMACOLOGIC EFFECTS:
Reduction of Heart Rate, Reduction of Ventricular Contraction, Reduction of Renin Release (β1) CLINICAL USE: Adjunctive Treatment of Hypertension, Alternative Treatment of Hypertension, Angina Pectoris, Dysrythmias, Myocardial Infarction SIDE EFFECTS: Bradycardia, Heart Failure, Bronchoconstriction, Inhibition of Glycogenolysis, Depression Extensive 1st pass metabolism in liver |
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Timolol
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PHARMACOLOGIC EFFECTS:
Reduction of Heart Rate, Reduction of Ventricular Contraction, Reduction of Renin Release (β1) CLINICAL USE: Adjunctive Treatment of Hypertension, Alternative Treatment of Hypertension, Congestive Heart Failure, Migraine Prophylaxis, Glaucoma SIDE EFFECTS: Bradycardia, Bronchoconstriction, Inhibition of Glycogenolysis |
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Pindolol
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PHARMACOLOGIC EFFECTS:
Reduction of Heart Rate, Reduction of Ventricular Contraction, Reduction of Renin Release (β1), Vasodilation (β2) CLINICAL USE: Adjunctive Treatment of Hypertension, Alternative Treatment of Hypertension SIDE EFFECTS: Bradycardia, Bronchoconstriction, Inhibition of Glycogenolysis |
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Metoprolol
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PHARMACOLOGIC EFFECTS:
Reduction of Heart Rate, Reduction of Ventricular Contraction, Reduction of Renin Release (β1) CLINICAL USE: Adjunctive Treatment of Hypertension, Alternative Treatment of Hypertension, Angina, Acute MI SIDE EFFECTS: Bradycardia, Depression |
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Bisoprolol
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PHARMACOLOGIC EFFECTS:
Reduction of Heart Rate, Reduction of Ventricular Contraction, Reduction of Renin Release (β1) CLINICAL USE: Adjunctive Treatment of Hypertension, Alternative Treatment of Hypertension, Chronic Heart Failure SIDE EFFECTS: Bradycardia, Hypotension |
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Nebivolol
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PHARMACOLOGIC EFFECTS:
Reduction of Heart Rate, Reduction of Ventricular Contraction (β1), Vasodilation (β2) CLINICAL USE: Adjunctive Treatment of Hypertension, Alternative Treatment of Hypertension SIDE EFFECTS: Bradycardia, Hypotension |
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Esmolol
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PHARMACOLOGIC EFFECTS:
Reduction of Heart Rate, Reduction of Ventricular Contraction (β1) CLINICAL USE: Emergency Tachycardia SIDE EFFECTS: Bradycardia, Hypotension Short half-life |
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Labetalol
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PHARMACOLOGIC EFFECTS:
Reduction of Heart Rate, Reduction of Ventricular Contraction (β1), Vasodilation (α1, β2,3) CLINICAL USE: Adjunctive Treatment of Hypertension, Alternative Treatment of Hypertension SIDE EFFECTS: Bradycardia, Hypotension |
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Carvedilol
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PHARMACOLOGIC EFFECTS:
Reduction of Heart Rate, Reduction of Ventricular Contraction (β1), Vasodilation (α1), Antioxidant, Anti-Proliferative CLINICAL USE: Adjunctive Treatment of Hypertension, Alternative Treatment of Hypertension, Chronic Heart Failure, Acute MI SIDE EFFECTS: Bradycardia, Hypotension |
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Effects of Angiotensin II
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Vasoconstriction, Constriction (Renal Efferent Arteriole), Increase Sodium reabsorption, INcrease aldosterone, ADH release (pituitary), Increase SNS activity, Vascular & Myocardial hypertrophy and hyperplasia
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Renin Inhibitor
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Aliskiren
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ACE Inhibitors
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Captopril, Lisinopril, Enalapril, Benazepril, Ramipril, Forsinopril
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Angiotesnin II-Receptor Antagonists
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Losartan, Candesartan, Irbesartan, Eprosartan, Telmesartan
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Bradykinin
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Physiological Antagonist of Angiotensin II (Vasodialation, Bronchoconstriction, Increase Vascular Permeability, Pain Mediation, Sodium Excretion)
Breakdown prevention by ACE Inhibitors |
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Drugs Associated with Bradykinin
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ICATIBANT: B2 antagonist used in pain, hyperalgesia, inflammation, bronchoconstriction
APROTININ: inhibit synthesis NSAIDS: Inhibit actions mediated by PG's |
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Endothelin
(Responses & Drugs) |
RESPONSES: Vasonconstriction, Contraction of non-vascular smooth muscle, "+" ionotropy, smooth muscle cell proliferation, cardiovascular regulation
DRUGS: Antagonists which treat Pulmonay HTN - Bosentan, Ambristan, Sitaxsentin |
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Endothelin
(ETa vs. ETb) |
ETa: activated PLC to form IP3 and DAG
ETb: stimulates PGI2 and NO production, causes a decrease in calcium release, promotes vasodilation and mitogen for cell proliferation |
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Atrial Natruiretic Peptide
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Release by atrial distension & in CHF
DRUGS: Nesiritide (tx for refractory heart failure), Ularitide (tx for decompensated heat failure); synthetic Urodilatin |
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Vasopeptidase Inhibitors
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Inhibits Neutral Endopeptidase (NEP - breaks down natriretic factors) & Angiotensin Converting Enzyme (ACE)
Causes decrease in Peripheral Resistance and Blood Pressure (Used in management of CHF) NEP Inhibitors: Omapatrilat, Sampatrilat, Fasidtrilat |
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Tachykinins
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Substance P - Perception/response through dorsal horn
Neurokinins A&B contract most smooth muscle DRUGS: Aprepitant - NK1 receptor antagonist (chemotherapy induced emesis) |
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Vasopressin
(Receptor Subtypes) |
V1=H2O Reabsoprtion in Kidney
V2=Vasoconstriction |
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Calcitonin Gene Related Peptide
(Where & Role) |
Found in CNS and PNS
Plays a role in Migraines (CN V) & peripheral cardiovascular regulation Potent Vasodilator |
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Neurotensin
(Where & Role) |
Found in CNS and GI Tract
NT/modulator in CNS (plays a role in Schizophrenia, Parkinson's & Drug Abuse) Regulate Acid/Pepsin Release & GI Motility |
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Vasoactive Intestinal Peptide
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Gs Coupled
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Adrenomedullin
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Physiological antagonist against endogenous vasoconstriction
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Urotensin
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Gq Coupled receptor producing vasoconstriction involved in HTN, Heart and/or Renal Failure, & DM
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Serotonin
(Effects on Neurons) |
Made from L-tryptophan
Metabolized from MAO to 5-hydroxyindoleaceticacid Regulates sleep, mood, appetite, temp, pain in CNS |
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Serotonin
(Effects on GI Smooth Muscle, Platelets, & Vasculature) |
GI SMOOTH MUSCLE: In enterochrommafin cells, stimulates GI motility
PLATELETS: Major Storage Site, Increase platelet aggregation VASCULATURE: Vasconstriction & Vasodilation (epithelial cells) |
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Serotonin
(In Diseases) |
AFFECTIVE DISORDERS: Depression, OCD, Anxiety
CARCINOID SYNDROME: Tumor of enterochromafin cells in GI tract (+++5-HT) VASCULATURE: Migraine HA's |
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5-HT1A
(Receptor Type & Agonist) |
RECEPTOR TYPE: Gi - decrease in cAMP/K channels
AGONIST: Buspirone (anxiety) |
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5-HT1D/B
(Receptor Type & Agonist) |
RECEPTOR TYPE: Gi - decrease in cAMP
AGONIST: Sumatriptan (migraine) |
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5-HT2A
(Receptor Type, Agonist, & Antagonist) |
RECEPTOR TYPE: Gq increase IP3 & DAG
AGONIST: LSD ANTAGONIST: Clozapine, Methysergide, Cyproheptadine |
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5-HT3
(Receptor Type & Antagonist) |
RECEPTOR TYPE: Na/K Chanel
ANTAGONIST: Ondansetron |
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5-HT4
(Receptor Type & Agonist) |
RECEPTOR TYPE: Gs - increase in cAMP
AGONIST: Cisapride |
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Iproniazid
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MAO Inhibitor
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Reserpine & Tetrabenazine
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Block Vesicle Formation
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Fluoxetine
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Re-uptake Blocker
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Ergot Alkaloid
(Receptor Selectivity) |
Bromocriptine (D-Receptor)
Ergonovine (α, 5-HT2 Receptor) Ergotamine (5-HT2, Uterine SM) LSD (D-Receptor, 5-HT CNS, Uterine SM) Methysergide |
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Effect of Ergot Alkaloids
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CNS - Hallucinations;
Dopamine receptor - prolactin release; Prolonged Vasocontriction (partial agonism and slow dissociation); Contraction of uterine sm (especially in pregnant uterus); "epinephrine reversal" |
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Clinical Uses of Ergot Alkaloids
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MIGRAINE (ergotamine, dihydroergotamine, methysergide)
HYPERPROLACTINEMIA (bromocriptine, cabergoline) POSTPARTUM HEMORRHAGE (ergonovine - never before delivery) Diagnosis of variant angina or cerebral insufficiency |
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PGI2
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Inhibit platelet aggregation
Produced by endothelin *Vasodilator Inhibit gastric acid secretion |
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PGE2
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Increased by pyrogens;
Vasodilator (HA in CNS); Reflec ionotropy; Relax non-pregnant uterus; Contract pregnant uterus; Increase blood & amniotic fluid during labor; Increase renal blood flow (vasodilate of afferent arteriole); Prevents reabsoption of H2O & Na; Increase renin secretion; Relax bronchial smooth muscle |
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PGF2
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Regression of corpus luteum;
Contracts non-preg/preg uterus; Important controller of parturition; Contract bronchial smooth muscle |
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TXA2
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Promotes platelet aggregation;
Vasoconstriction; Contract bronchial smooth muscle |
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Pharmacology of Prostaglandins
Glaucoma |
1. Latanoprost
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Pharmacology of Prostaglandins
Gastric & Duodenal Ulcers |
Misoprostol
Misoprostol/Diclofenac (ulcers in patients on high doses of NSAIDS) |
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Pharmacology of Prostaglandins
1.Abortion 2.Postpartum Hemorrhage 3. Labor Induction |
ABORTION: Misoprostol, Carboprost Tromethamine, Dinoprostone
POSTPARTUM HEMORRHAGE: Carboporst Tromethamine LABOR INDUCTION: Dinoprostone, Carboprost Tromethamine |
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Pharmacology of Prostaglandins
Cardiovascular/Respiratory 1. Patent Ductus Arteriosis 2. Erectile Dysfunction 3. Pulmonary Hypertension |
PATENT DUCTUS ARTERIOSIS: Alprostadil
ERECTILE DYSFUNCTION: Alprostadil PULMONARY HTN: Epoprostanol, Iloprost, Treprostinil |
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Functions of Leukotrienes on Cardiovascular System
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Coronary artery constriction;
Pulmonary artery constriction; Increased permeability; Mediator of endotoxic shock (bronchoconstriction, vasoconstriction, impaired cardiac fcn, capillary leakage) |
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Functions of Leukotrienes on Leukocytes
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LTB4 - chemotactic for neutro, eosinophils, & monocytes
Promotes PMN aggregation and degranulation |
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Functions of Leukotrienes on Renal System
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Produces Acute Glomerular Nephritis;
Venoconstriction leading to decreased GFR |
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Functions of Leukotrienes on Pulmonary System
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LTC4 & LTD4 - mediators of asthma and hypersensitivity;
Produced by mast cells to Ab challenge; Bronchial SM constirction; Increased edema & mucous |
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Zafirlukast
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LTD4/LTE4 Receptor Antagonist;
Inhibits bronchoconstriction (maintenance for chronic asthma); Metabolized by CYP2C9 (Inhibits *CYP3A4* & CYP2C9) |
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Montelukast
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LTD4 Antagonst;
Inhibits bronchoconstriction (maintenance of chronic asthma, & exercise induced asthma); SIDE EFFECTS: Suicidal Ideation, Mood Changes |
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Zileuton
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5-Lipoxygenase inhibitor (blocks LT synthesis);
Chronic Asthma; Inhibits Cytochrome P450 System (reduces clearance of drugs) |
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Functions of Platelet Activating Factor (PAF) in Pulmonary System
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Bronchoconstiction (last 4 weeks)
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Functions of Platelet Activating Factor (PAF) in Cardiovascular System
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Hypotension (independent of SNS)
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Functions of Platelet Activating Factor (PAF)
(Other) |
Platelet Aggregation;
Chemotaxis; IV=anaphylaxis; Successful implantation and pregnancy; Release rxn in phagocytes |
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Pathophysiological Functions of PAF
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Shock;
Asthma (Bronchoconstriction); Inflammation; Anaphylaxis; Graft Rejection |
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H1 Receptor
Type, Distribution, Response |
TYPE: Gq Receptor
DISTRIBUTION: Vascular SM, Endotheliium, Non-vascular SM, exocrine glands, CNS RESPONSE: Vasodilation, edema, NO production, bronchoconstriction, pruritus, cough reflex, Increase secretions, wakefulness |
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H2 Receptor
Type, Distribution, Response |
TYPE: Gs
DISTRIBUTION: Gastric Mucosa & Heart RESPONSE: Increase gastric acid secretion, Increase heart rate and contractility directly |
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H3 Receptors
Type, Distribution, Response |
TYPE: Gi
DISTRIBUTION: presynaptic nerve terminals RESPONSE: Decrease neurotransmitter release |
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H4 Receptors
Type, Distribution, Response |
TYPE: Gi
DISTRIBUTION: Blood Cells and CD4 T cells RESPONSE: Histamine mediated cytokine production |
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H1 Receptor Agonists
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Ethanolamines, Alkylamines, Ethylaminediamines, Phenthiazines, Piperazines, Piperidines
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1st Generation Antihistamines
(Ethanolamines) S=sedative, E=anti-emetic, C=anti-cholinergic, MS=morning sickness, I=insomnia |
ANTI-EMETICS/MOTION SICKNESS
Clemastine - S, C (not motion sickness/nor anti-emetic) Dimenhydrinate - S, E, C, Diphenhydramine - S, E, C, MS, I Carbinoxamine - S, E, C Doxylamine - S, E, C, MS |
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1st Generation Antihistamies
(Alkylamines) S=sedative, E=anti-emetic, C=anti-cholinergic |
OTC COLD REMEDIES
Brompheniramine - S, C Chlorpheniramine - S, C Tripolidine - S, C Dry you up & put you to sleep |
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1st Generation Antihistamines
(Ethylaminediamines) S=sedative, E=anti-emetic, C=anti-cholinergic |
Pryilamine - C
Tripelennamine - S, C |
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1st Generation Antihistamines
(Phenothiazines) S=sedative, E=anti-emetic, C=anti-cholinergic |
ANTI-EMETIC
Promethazine - S, E, C |
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1st Generation Antihistamines
(Piperazines) S=sedative, E=anti-emetic, C=anti-cholinergic |
ANTI-EMETICS
Meclizine - S, E, C (vertigo) Cyclizine - S, E, C Hydroxyzine - S, E, C (anxiety, psychosis related tension) Category D Drug |
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2nd Generation Anti-Histamines
(Piperazines) S=sedative, E=anti-emetic, C=anti-cholinergic |
Citirizine - S
Mildly sedative, Category D drug |
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1st Generation Antihistamine
Intranasal S=sedative, E=anti-emetic, C=anti-cholinergic |
Azelastine - S
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1st Generation Antihistamine
(Piperidines) S=sedative, E=anti-emetic, C=anti-cholinergic |
Cyproheptadine - S, C
5-HT Antagonist Non-Sedative (doesn't cross BBB) |
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2nd Generation Antihistamines
(Piperidines) S=sedative, E=anti-emetic, C=anti-cholinergic |
Loratidine -
Fexofenadine - S Non-sedative (doesn't cross BBB) |
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H1 Receptor Antagonist Therapeutic Uses
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Allergic Reactions
Motion Sickness & Vestibular Disturbances Sleep Aids Nausea/Vomiting in Pregnancy (not piperazines) Antiparkinsonism |
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H1 Receotor Antagonists
Adverse Effects & Drug Interactions |
ADVERSE EFFECTS: Hyperexcitability (infants and elderly), Sedation, Dry Mouth
DRUG INTERACTIONS: metabolized by CYP3A4 (QT Syndrome when combined w/other drugs affecting cardiac K channels) |
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H2 Receptor Antagonists
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Cimetidine, Ranitidine, Nizatidine
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H2 Receptor Antagonist Therapeutic Effects
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GI ISSUES: Peptic Duodenal Ulcers, Gastric Ulcer, GERD, Hypersecretory conditions, (possible hiatal hernia, stress induced ulcer, or iatrogenic ulcer)
Decrease gastric acid secretion |
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H2 Receptor Antagonist Side Effects
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CNS: Confusion, slurred speech (paradoxical excitement in young & old)
ANDROGENIC EFFECTS: (Cimetadine Only) Gynecomastia (males), Galactorrhea (females), Decrease sperm and impotence Blood dyscrasias, Reversible hepatitis (ranitidine), Abnormalities in liver enzymes (famotidine, nizatidine) |
