Drugs Flashcards
Achetylcholine
Type: Cholinergic
Subtype: Choline Ester
Target Receptor/Enzyme: Non-selective for Muscarinic & Nicotinic Receptors
Mechanism of Action: Direct Acting Muscarinic & Nicotinic Agonist
Main Function: Miosis during sx
Therapeutic Use: Rapid miosis after cataract sx
Contraindications/Side Effects: Sweating, salivation, flushing, low bp, nausea, abdominal pain, diarrhea, bronchoconstriction
Notes: Quaternary ammonium, lipophobic, rapidly hydrolyzed, no systemic effects, not widely used clinically
Bethanechol
Type: Cholinergic
Subtype: Choline Ester
Target Receptor/Enzyme: M3
Mechanism of Action: Direct Acting Muscarinic Agonist
Main Function: Smooth muscle relaxation & Vasodilation
Therapeutic Use: post-op urinary retention, atony of bladder
Contraindications/Side Effects:
Notes:
Methacholine
Type: Cholinergic Subtype: Choline Ester Target Receptor/Enzyme: M2 Mechanism of Action: Direct Acting Muscarinic Agonist Main Function: Bronchoconstriction Therapeutic Use: Test bronchoconstriction in asthma-suspecting patients Contraindications/Side Effects: Notes: resistant to hydolysis by AChE
Pilocarpine
Type: Cholinergic
Subtype: Natural Alkaloids
Target Receptor/Enzyme:
Mechanism of Action: Direct-Acting Partial Muscarinic Agonist
Main Function: Miosis
Therapeutic Use: Glaucoma & Dry mouth after radiotherapy, CF Diagnostics
Contraindications/Side Effects: Sweating, Salivation, Flushing, Low bp, Abdominal pain, Nausea, Diarrhea, Bronchospasm
Notes: Tertiary amine, Lipophilic
Nicotine
Type: Cholinergic
Subtype: Natural Alkaloid
Target Receptor/Enzyme:
Mechanism of Action: Direct-Acting Nicotinic Agonist
Main Function: Low doses - stimulates autonomic ganglia High doses - ganglionic & neuromuscular block —> paralysis
Therapeutic Use: Smoking cessation therapy
Contraindications/Side Effects: Addiction
Notes: Tertiary Amine, Lipophilic
Edrophonium
Type: Cholinergic Subtype: Target Receptor/Enzyme: Mechanism of Action: Indirect Acting / AChE Inhibitor or Anticholinesterase Main Function: Therapeutic Use: Myasthenia Gravis Diagnosis; Reverse neuromuscular block Contraindications/Side Effects: Notes:
Physostigmine
Type: Cholinergic Subtype: Carbamate Target Receptor/Enzyme: Mechanism of Action: Acetylcholinesterase Inhibitor / Indirect Main Function: Therapeutic Use: Anticholinergic OD Contraindications/Side Effects: Notes: can enter CNS, Lipophilic
Neostigmine
Type: Cholinergic Subtype: Carbamate Target Receptor/Enzyme: Mechanism of Action: Acetylcholinesterase Inhibitor / Indirect Main Function: Therapeutic Use: Myasthenia Gravis Tx, Urinary retention, reverse neuromuscular block Contraindications/Side Effects: Notes:
Pyridostigmine
Type: Cholinergic Subtype: Carbamate Target Receptor/Enzyme: Mechanism of Action: Indirect / Acetylcholinesterase Inhibitor Main Function: Therapeutic Use: Myasthenia Gravis tx Contraindications/Side Effects: Notes:
Malathion
Type: Cholinergic Subtype: Organophosphate Target Receptor/Enzyme: Mechanism of Action: Indirect Acting / Acetylcholinesterase Inhibitor Main Function: Therapeutic Use: Insecticides Contraindications/Side Effects: Poisonous Notes:
Sarin
Type: Cholinergic Subtype: Organophosphate Target Receptor/Enzyme: Nerve Agent Mechanism of Action: Indirect / AChE inhibitor Main Function: Therapeutic Use: Contraindications/Side Effects: Toxic Notes:
Atropine
Type: Cholinergic
Subtype: Belladonna Alkaloid
Target Receptor/Enzyme: Muscarinic Antagonist
Mechanism of Action:
Main Function: Mydriasis & Cycloplegia; Decrease secretions, gastric motility, hypermotility of bladder; Tachycardia
Therapeutic Use: Block secretions before sx; Cholinergic agonist OD (antidote)
Contraindications/Side Effects: Dry mouth, Blurred vision, Sandy eyes, Tachycardia, Constipation, Urinary retention, Restlessness, Confusion, Hallucinations, Delirium, Anhydrosis, Increase body temperature
Notes: Lipophilic
Scopolamine
Type: Cholinergic Subtype: BellaDonna Alkaloid Target Receptor/Enzyme: Muscarinic Antagonist Mechanism of Action: Main Function: Therapeutic Use: Prevent motion sickness Contraindications/Side Effects: Angle-closure glaucoma, prostatic hypertrophy, elderly Notes:
Ipratropium
Type: Cholinergic Subtype: Target Receptor/Enzyme: Muscarinic Antagonist Mechanism of Action: Main Function: Therapeutic Use: COPD & Asmtha Tx Contraindications/Side Effects: Notes:
Tropicamide
Type: Cholinergic Subtype: Target Receptor/Enzyme: Muscarinic Antagonist Mechanism of Action: Main Function: Mydriasis Therapeutic Use: Fundoscopy Contraindications/Side Effects: Notes: Lipophilic
Hexamethonium
Type: Cholinergic Subtype: Target Receptor/Enzyme: N(n) Mechanism of Action: Ganglion Blocker - Muscarinic Antagonist Main Function: Therapeutic Use: Contraindications/Side Effects: Tachycardia Notes:
Tubocurarine
Type: Cholinergic Subtype: Target Receptor/Enzyme: (Nm) Mechanism of Action: Neuromuscular Blocker - Muscarinic Antagonist Main Function: relax muscle Therapeutic Use: anesthesia in sx Contraindications/Side Effects: Notes:
Succinylcholine
Type: Cholinergic Subtype: Target Receptor/Enzyme: Mechanism of Action: Neuromuscular Block - Muscarinic Antagonist Main Function: Therapeutic Use: rapid intubation; depression Contraindications/Side Effects: Notes:
Botulinum Toxin
Type: Cholinergic Subtype: Target Receptor/Enzyme: Mechanism of Action: Acts Presynaptically - Cholinergic Antagonist Main Function: Inhibits ACh release Therapeutic Use: Muscle spasms; facial wrinkles, hyperhidrosis Contraindications/Side Effects: Notes:
Norepinephrine
Type: Adrenergic Subtype: Direct Acting Endogenous Catecholamine Target Receptor/Enzyme: A1, A2, B1 Main Function: Peripheral Vasoconstriction; Increase BP: Increase Cardiac Contractility Mechanism of Action: Endogenous agonist Therapeutic Use: Shock Contraindications/Side Effects: Notes:
Epinephrine
Type: Adrenergic
Subtype: Direct Acting Endogenous Catecholamine
Target Receptor/Enzyme: Alpha & Beta receptors
Main Function: Increase HR & contractile force & CO; Increase O2 demand; Increase Renin release; Arteriole constriction; Dilate skeletal muscle blood vessels; Bronchodilation; Increase liver glycogenolysis; Increase lipolysis
Mechanism of Action: At [low]=B1&B2, Bronchodilation. At [high]=A1, Vasoconstriction, Increase BP
Therapeutic Use: Anaphylactic shock, Acute Asthma attack, Cardiac arrest
Contraindications/Side Effects:
Notes:
Isoproterenol
Type: Adrenergic Subtype: Non-Selective Beta Agonist Target Receptor/Enzyme: B1 & B2 Main Function: Increase HR/contractile force/CO; Dilate arterioles of skeletal muscle/Decrease resistance; Decrease Diastolic Pressure; Stable or Increase Systolic Pressure; Decrease MAP; Bronchodilation Mechanism of Action: Therapeutic Use: Stimulate HR during emergency heart block or bradycardia Contraindications/Side Effects: Notes:
Dobutamine
Type: Adrenergic Subtype: B1 Agonist Target Receptor/Enzyme: B1 Main Function: Mild Vasodilation; Increase O2 consumption Mechanism of Action: Therapeutic Use: Stress Echocardiogram; Acute Heart Failure Management; Cardiogenic Shock Management Contraindications/Side Effects: Notes:
Albuterol
Type: Adrenergic Subtype: B2 Agonist Target Receptor/Enzyme: B2 Main Function: Bronchodilation Mechanism of Action: Therapeutic Use: Acute Asthma Attacks Contraindications/Side Effects: Notes:
Phenylephrine
Type: Adrenergic Subtype: A1 Agonist Target Receptor/Enzyme: A1 Main Function: Vasoconstriction Mechanism of Action: Therapeutic Use: Nasal Decongestant; Mydriatic Contraindications/Side Effects: Notes:
Clonidine
Type: Adrenergic
Subtype: Partial A2 Agonist
Target Receptor/Enzyme: A2
Main Function: Centrally-Acting Hypertensive
Mechanism of Action: Activates central presynaptic A2 adenoreceptors
Therapeutic Use: Reduce symapthetic outflow —> Decrease BP
Contraindications/Side Effects:
Notes: Acts on Gi (inhibitory receptor)
Amphetamine
Type: Adrenergic
Subtype: Indirect Acting Releasing Agents
Target Receptor/Enzyme: Cause NE release of presynaptic terminal, potentiate NE effects
Main Function: Increase BP
Mechanism of Action: Central stimulatory action
Therapeutic Use: ADHD; Narcolepsy
Contraindications/Side Effects:
Notes:
Tyramine
Type: Adrenergic
Subtype: Indirect Acting Releasing Agent
Target Receptor/Enzyme: Causes NE release from presynaptic vessicles
Main Function:
Mechanism of Action: Normally oxidized my MAO
Therapeutic Use:
Contraindications/Side Effects:
Notes: Vasopressin episode in Anti-Depressant patient; In fermented foods
Cocain
Type: Adrenergic
Subtype: Indirect Acting Uptake Inhibitor
Target Receptor/Enzyme:
Main Function: potentiation & prolongation of central & peripheral actions
Mechanism of Action: Blocks monoamine reuptake so accumulation in synaptic cleft
Therapeutic Use:
Contraindications/Side Effects:
Notes:
Ephedrine
Type: Adrenergic Subtype: Mixed Acting Target Receptor/Enzyme: Increase NE release, Activate adrenergic receptors Main Function: Mechanism of Action: Penetrates CNS Therapeutic Use: Pressor agent during spinal anesthesia Contraindications/Side Effects: Notes: Not a catecholamine
Pseodoephedrine
Type: Adrenergic Subtype: Mixed Acting Agonist Target Receptor/Enzyme: Ephedrine enantiomer Main Function: Mechanism of Action: Therapeutic Use: Decongestant Contraindications/Side Effects: Notes:
Phenoxybenzamine
Type: Adrenergic
Subtype: Non-Selective Alpha Antagonist
Target Receptor/Enzyme: A1&A2
Main Function: Reduces sympathetic tone of BV; Decrease PVR
Mechanism of Action: Irreversible antagonist
Therapeutic Use: Pheochromocytoma Surgery Removal
Contraindications/Side Effects:
Notes:
Phentolamine
Type: Adrenergic Subtype: Non-Selective A-Antagonist Target Receptor/Enzyme: A1&A2 Main Function: Mechanism of Action: Therapeutic Use: Pheochromocytoma surgery - control hypertension; Hypertensive crisis due to stimulant drug overdose Contraindications/Side Effects: Notes:
Prazosin
Type: Adrenergic Subtype: A1-Selective Antagonist Target Receptor/Enzyme: A1 Mechanism of Action: Relax arterial & venous smooth muscle Main Function: Lower BP Therapeutic Use: Hypertension (not DOC); BPH - relax smooth muscle in bladder, prostate, urethra, which improves urine flow Contraindications/Side Effects: Notes:
Propranolol
Type: Adrenergic
Subtype: Non-Selective Beta Antagonist
Target Receptor/Enzyme: B1&B2
Mechanism of Action:
Main Function: Decrease HR/contractility; Respiratory crisis; Decrease glycogenolysis; Decrease glucagon secretion
Therapeutic Use: Hypertension; Hyperthyroidism; Performance Anxiety; Stable Angina Pectoris; Glaucoma; Atrial Fibrillation; MI; Migraine Prophylaxis
Contraindications/Side Effects: Bronchoconstriction in asthmatics; Hypoglycemia in insulin-dependent diabetics
Notes: CNS effects: Sedation; Dizziness; Lethargy; Fatigue
Atenolol
Type: Adrenergic Subtype: B1 Selective Antagonist Target Receptor/Enzyme: B1 Mechanism of Action: Main Function: Decrease HR/contractility Therapeutic Use: Hypertensive Diabetic Patients Contraindications/Side Effects: Bronchospasm but not likely Notes:
Pindolol
Type: Adrenergic
Subtype: Non-selective beta antagonist
Target Receptor/Enzyme: B1 & B2
Mechanism of Action: Partial agonist - acts as competitive reversible antagonist
Main Function: Decrease HR/contractility; Decrease glycogenolysis; Decrease glucagon secretion
Therapeutic Use: Hypertensive patients with diminished cardiac reserve or propensity to bradycardia
Contraindications/Side Effects:
Notes:
Sulfonamide/Sulfa Drugs
Antibiotic
Inhibit PABA, Para Amino Benzoic Acid
Folate Analogue - inhibits folic acid synthesis
Trimethoprim
Antibiotic
Inhibits Dihydrofolate reductase
Methotrexate
Anti-Cancer
Competitively inhibits Dihydrofolate reductase in mammalian cells
Uses: Tx of psoriasis, RA, arthritis
Side effects: anemia, scaly skin, hair loss, immune deficiency, GI disturbance
Mycophenoic Acid
Inhibits IMP dehydrogenase (formation of GTP and ATP)
Hydroxyurea
Inhibits ribonucleotide reductase (conversion of ADP/GDP to ATP/GTP)
Allopurinol
Irreversibly inhibits xanthine oxidase
Decrease uric acid formation
Increase Hypoxanthine and Xanthine in the blood
Uses: Gout tx
Febuxostat
Uses: gout tx
Mechanism of action: xanthine oxidase inhibitor
Probenecid
Uses: gout tx
Mechanism of action: increase excretion of uric acid
5 Fluorouracil
Anti cancer ; Suicide inhibitor
Irreversibly binds Thymidylate Synthetase
Inhibits conversion of dUMP to dTMP
