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