Drugs Flashcards
Isoniazid
Anti-tuberculosis drug metabolized by N-acetyltransferase-2
Anti-depressants
Metabolized by CYP2D6
Omeprazole, Phenytoin, Clopidogrel
Metabolized by CYP2C19
Warfarin
Metabolized by CYP2C9
- A vitamin K antagonist that inhibits Vitamin K epoxide reductase complex (VKORC1)
Succinylcholine
a depolarizing muscle relaxant - treatment affected by pseudocholinesterase polymorphism
Mercaptopurine
Bone marrow suppression in cancer treatment
- treatment affected by TPMPT polymorphism
Digoxin
Cardiac glycoside - Treatment affected by P-glycoprotein polymorphism
Norepinephrine Classification: Receptor activity: Cardiovascular effects: Therapeutic Uses:
Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor activity: α1, (α2, β1)
Cardiovascular effects: Peripheral vasoconstriction - increase PVR; Increase BP; reflex bradycardia
Therapeutic Uses: Used as vasoconstrictor under intensive care situations (shock); Increase BP during reduced sympathetic tone
Epinephrine Classification: Receptor activity: Cardiovascular effects: Respiratory: Metabolic: Therapeutic Uses:
Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor activity: α1, α2, β1, β2
Cardiovascular effects: Increase HR, contractile force, CO; Increase SBP, decrease DBP; Decrease PVR; Constriction of vascular beds but dilation of skeletal muscle vessels
Respiratory: Bronchodilation
Metabolic: Hyperglycemia and Lypolysis
Therapeutic Uses: Rapid relief of hypersensitivity reactions to drugs and other allergens; Co administered with local anesthetics to increase duration of action
Isoproterenol Classification: Receptor activity: Cardiovascular effects: Respiratory: Therapeutic Uses:
Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor activity: β1, β2
Cardiovascular effects: Decrease peripheral resistance; increase HR, contractile force, CO; Decrease mean BP
Respiratory: Bronchodilation
Therapeutic Uses: In emergencies to stimulate heart rate during bradycardia
Dopamine Classification: Receptor selectivity: Cardiovascular (Dose-Dependent): Therapeutic Uses:
Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor selectivity: DA1, β1, α1
Cardiovascular (Dose-Dependent):
- Low dose - vasodilation of renal and mesenteric arteries - decrease peripheral resistance (DA1)
- Medium dose - Increase heart rate, contractile force, cardiac output (β1)
- High dose - Vasoconstriction and increase peripheral resistance (α1)
Therapeutic Uses: Severe decompensated heart failure, shock
Dobutamine Classification: Receptor Selectivity: Cardiovascular: Therapeutic Uses:
Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor Selectivity:
-(-) dobutamine - α1 agonist and β agonist
-(+) dobutamine - α1 antagonist and β agonist
Overall effect as β1 agonist
Cardiovascular:
- Increased cardiac rate, contractility and output
- Minimal change in peripheral resistance and blood pressure
Therapeutic Uses: Short term treatment of cardiac decompensation; Cardiac stress testing
Methyldopa Classification: Receptor Selectivity: Cardiovascular: Major Therapeutic Use: Side Effects:
Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor Selectivity: Stimulate CNS α2 receptors (Inhibit sympathetic outflow)
Cardiovascular: Decreases PVR, HR and CO
Major Therapeutic Use: Anti-hypertensive
Side Effects: Sedation; dry mouth, edema, rebound hypertension
Phenylephrine Classification: Receptor selectivity: Cardiovascular: Therapeutic Use:
Class: Direct Acting Adrenergic Agonists - Non-Catecholamine
Receptor selectivity: α1 agonist
Cardiovascular: Increases SBP and DBP; Decreases HR (reflex); Decrease blood flow
Therapeutic Use: Nasal decongestant; used with local anesthetics to increase duration of action; treatment of hypotension
Clonidine Classification: Receptor selectivity: Cardiovascular: Therapeutic Use:
Classification: Direct Acting Adrenergic Agonists - Non-Catecholamine
Receptor selectivity: CNS α2 agonist
Cardiovascular: Prolonged BP lowering, Decrease PVR, HR and CO
Therapeutic Use: Anti-hypertensive agent
Albuterol Classification: Receptor selectivity: Therapeutic Use: Side Effects:
Classification: Direct Acting Adrenergic Agonists - Non-Catecholamine
Receptor selectivity: Act mainly on β2 adrenergic receptors (short acting)
Therapeutic Use: Bronchodilator
Side Effects: Tremor, anxiety, tachycardia
Salmeterol Classification: Receptor selectivity: Therapeutic Use: Onset:
Classification: Direct Acting Adrenergic Agonists - Non-Catecholamine
Receptor selectivity: β2 agonist
Therapeutic Use: Chronic obstructive pulmonary disease, asthma
Onset: Slow onset of action; long duration of action (w/ inhalation)
Tyramine: Classification: Action: Metabolized: Source:
Classification: Indirect acting adrenergic agonist
Action: Releases NE from sympathetic nerves
Metabolized: to inactive products by MAO
Source: High levels in fermented foods
Amphetamine Classification: Receptor Activation: Action: Therapeutic Use:
Classification: Mixed acting adrenergic agonist
Receptor Activation: Peripheral α and β receptor actions, and also weak direct α and β agonist
Action: Releases NE from adrenergic neurons; weakly blocks NET; depresses appetite
Therapeutic Use: Narcolepsy; ADD
Ephedrine: Class: Receptor Activation: Action: Therapeutic use:
Class: Mixed acting adrenergic agonist
Receptor Activation: α and β receptor direct agonist
Action: Releases NE and CNS stimulation
Therapeutic use: Previously used to treat asthma but has been replaced by β2 agonists
Pseudoephedrine Class: Receptor Activation: Action: Therapeutic use:
Class: Mixed acting adrenergic agonist
Receptor Activation: Direct α1 agonist activity with little β2 agonist activity
Action: Orally effective but less CNS stimulation - precursor to Methamphetamine
Therapeutic use: Nasal decongestant
Guanethidine/Guanadrel Class: Action: Therapeutic Use: Side Effects:
Class: Adrenergic antagonist (neuron blocker)
Action: Inhibits NE release, and deplete neuronal amine stores - Taken into adrenergic nerves by NET; effects inhibited by tricyclic antidepressants that also inhibit the NET
Therapeutic Use: Orally active compounds used to treat severe hypertension
Side Effects: Numerous, limit use, interferes w/ sexual function
Reserpine Class: Action: Therapeutic Use: Side Effects:
Class: Adrenergic antagonist (Neuron blocker)
Action: Diffuses into adrenergic nerves (w/o NET) and depletes neurotransmitters - inhibits VMAT2
Therapeutic Use: Orally active compound used to treat essential hypertension
Side Effects: Depression, suicide, sedation
Phenoxybenzamine Class: Receptors blocked (mechanism): Action: Therapeutic Use:
Class: Adrenergic antagonist (Receptor blocker)
Receptors blocked (mechanism): α1 and α2 receptors; irreversible antagonist
Action: Produces vasodilation porportional to degree of sympathetic tone (Long duration of action)
Therapeutic Use: pheochromcytoma
Phentolamine: Class: Receptors blocked (mechanism): Action: Therapeutic Use:
Class: Adrenergic antagonist (Receptor blocker) Receptors blocked (mechanism): α1 and α2 receptors; competitive reversible antagonist Action: Block can be overcome by increasing levels of agonists (short duration of action) Therapeutic Use: Hypertension; Pheochromcytoma; Reverses or shortens the duration of soft tissue anesthesia produced by combined local anesthetic and sympathomimetic
Prazosin Class: Receptors blocked (mechanism): Action: Therapeutic Use: Side effects:
Class: Adrenergic antagonist (Receptor blocker)
Receptors blocked (mechanism): α1 (α2); competitive antagonist
Action: Minimal tachycardia; decreases vascular tone in resistance and and capacitance beds; produces less LDL and more HDL
Therapeutic Use: Hypertension; short term congestive heart failure; Benign protostatic hyperplasia
Side Effects: First dose phenomenon - hypotension and syncope 30-90 minutes after first dose
Tamsulosin Class: Receptors blocked (mechanism): Action: Therapeutic Use:
Class: Adrenergic antagonist (receptor blocker)
Receptors blocked (mechanism): α1 (with selectivity for α1A receptors over α1B receptors)
Action: Acts on α1 receptors in prostate
Therapeutic Use: Effective treatment for BPH
Propanolol Class: Receptors blocked (mechanism): Therapeutic Use: Side Effects:
Class: Adrenergic receptor antagonist (First generation)
Receptors blocked (mechanism): β1 and β2 receptors (Competitive reversible antagonist)
Therapeutic Use: Hypertension; angina; Cardiac arrhythmias due to excess catecholamines; migraine prophylaxis
Side Effects: Cardiac depression, bradycardia/heart block; may increase airway resistance
Timolol
Class:
Receptors blocked (mechanism):
Therapeutic Use:
Class: Adrenergic Receptor Antagonist (First Generatio)n
Receptors blocked (mechanism): Non selective β
Therapeutic Use: Same as propanolol; also used in treatment of wide angle glaucoma
Metoprolol
Class:
Receptors Blocked:
Therapeutic Use:
Class: Adrenergic Receptor Antagonist (Second generation)
Receptors Blocked: β1 (Competitive reversible)
Therapeutic Use: Same as propanolol; also used to treat heart failure
Atenolol
Class:
Therapeutic Use:
Action:
Class: Adrenergic Receptor Antagonist (Second Generation)
Therapeutic Use: Similar to popanolol (except for migrain prophylaxis)
Action: Does not penetrate into CNS – less CNS side effects
Labetalol
Class:
Receptors blocked:
Therapeutic Use:
Class: Adrenergic Receptor Antagonist (Third Generation)
Receptors blocked: α1 receptor and both β receptors (competitive antagonist)
Therapeutic Use: Essential hypertension (oral) and hypertensive emergencies (IV)
Carvedilol Class: Receptors blocked: Actions Therapeutic Use:
Class: Adrenergic Receptor Antagonist (Third Generation)
Receptors blocked: α1 receptor and both β receptors (competitive antagonist)
Actions: Blocks L-type Calcium channels at higher doses
Therapeutic Use: Chronic heart failure, hypertension, and acute MI
Acetycholine
Choline ester: Opthalmic for rapid miosis
Bethanechol Classification: Primary Effect: Therapeutic Uses: Side Effects:
Classification: Muscarinic Agonist - Choline Esters
Primary Effect: G.I/G.U system
Therapeutic Uses: Orally or subcutaneous for urinary retention in the absence of obstruction
SE: SLUDGE, hypotension, bradycardia, blurred vision
Muscarine
Present in some species of mushrooms
Pilocarpine:
Classification:
Therapeutic Uses:
Side Effects:
Classification: Muscarinic Agonist - Alkaloid
Therapeutic Uses: Orally for xerostomia
- Miotic agent used opthalmically to treat wide-angle glaucoma as well as emergency treatment for narrow angle glaucoma
SE: SLUDGE, hypotension, bradycardia, blurred vision
Edrophonium Classification: Administration: Therapeutic Use: Side Effects:
Classification:Reversible Acetylcholinesterase Inhibitor
Administration: IV
Therapeutic Use: Diagnosis of myasthenia gravis
- Distinguish cholinergic from myasthenic crisis
- Reverse paralysis by competitive neuromuscular blocking agents
SE: SLUDGE, hypotension, bradycardia, blurred vision
Physostigmine
Class:
Therapeutic Use:
Side Effects:
Class: Reversible Acetylcholinesterase Inhibitor
Therapeutic Use: Treatment of chronic wide-angle glaucoma
- Toxicity by antimuscarinic drug poisoning - penetrates CNS
SE: SLUDGE, hypotension, bradycardia, blurred vision
Neostigmine
Class:
Therapeutic Use:
Side Effects:
Class: Reversible Acetylcholinesterase Inhibitor
Therapeutic Use: Treatment of myasthenia gravis (oral)
- Prevention and treatment of post-operative atony of gut and bladder
- Reversal of paralysis by neuromuscular junction blocking agents
SE: SLUDGE, hypotension, bradycardia, blurred vision
Nerve Gas
Class:
Toxicity:
Sarin
Class: Organophosphate
Toxicity: SLUDGE, medullary respiratory center depression, muscle paralysis due to depolarizing neuromuscular junction blockade
Insecticide
Class:
Toxicity:
Malathion - Detoxified in humans
Class: Organophosphate
Toxicity: SLUDGE, medullary respiratory center depression, muscle paralysis due to depolarizing neuromuscular junction blockade
Atropine
Class:
Therapeutic Use:
Class: Muscarinic receptor antagonist - Alkaloid
Therapeutic Use: Bradyarrhythmias
- Opthalmic uses: mydriasis and cycloplegia
- Blocks vagal reflexes and secretions during anesthesia
- Acetylcholinesterase and muscarinic toxicity
Pralidoxime
Therapeutic Use:
Therapeutic Use: Reactivates Ach peripherally (2-3 hours)
Scopolamine
Classification:
Therapeutic Uses:
Classification: Muscarinic Receptor Antagonist - Alkaloid
Therapeutic Uses: Motion sickness and vestibular diseases (penetrates CNS)
Ipratropium
Class:
Therapeutic Uses:
Class: Muscarinic Receptor Antagonists - Semi-synthetic derivatives
Therapeutic Use: COPD (less effective for asthma)
Tropicamide
Class:
Therapeutic Use:
Class: Muscarinic Receptor Antagonists
Therapeutic Use: Mydriatic and cycloplegic
Oxybutynin
Class:
Therapeutic Use:
Side Effects:
Class: Muscarinic Receptor Antagonist
Therapeutic Use: Overactive bladder, incontinence
SE: xerostomia, blurred vision, constipation, drowsiness
Darifenacin
Class:
Therapeutic Use:
Class: Muscarinic Receptor Antagonist
Therapeutic Use: Overactive bladder, incontinence
Glycopyrrolate
Class:
Therapeutic:
Class: Muscarinic Receptor Antagonist
Therapeutic Use: Used to block parasympathetic effects when neostigmine is used to reverse skeletal muscle paralysis by neuromuscular blocking agents
Muscarinic Receptor Antagonist: Side Effects
Hot as hare Dry as bone Red as a beet Blind as a bat Drowsiness Mad as a hatter
Rocuronium Class: Duration of Action: Elimination: CV effects: Histamine release:
Class: Competitive Neuromuscular Blocking Agents
Duration of Action: Intermediate (30-60 minutes)
Elimination: Liver metabolism
CV effects: Minimal
Histamine release: None
Atracurium Class: Duration of Action: Elimination: CV effects: Histamine release:
Class: Competitive Neuromuscular Blocking Agents
Duration of Action: Intermediate (30-60 minutes)
Elimination: Spontaneously degrades in plasma
CV effects: Minimal
Histamine release: Slight
Vercuronium Class: Duration of Action: Elimination: CV effects: Histamine release:
Class: Competitive Neuromuscular Blocking Agents
Duration of Action: Intermediate (60-90 minutes)
Elimination: Liver metabolism
CV effects: Minimal
Histamine release: None
Pancuronium Class: Duration of Action: Elimination: CV effects: Histamine release:
Class: Competitive Neuromuscular Blocking Agents
Duration of Action: Long (120-180 minutes)
Elimination: Renal excretion
CV effects: Slight increase in HR and BP
Histamine release: Slight
Succinylcholine
Class:
Theraputic use:
Metabolized by:
Class: Depolarizing Neuromuscular Blocking
Therapeutic Use: Produces muscle fasciculations and then paralysis
Metabolized by: Pseudocholinesteraese
