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BMD 315- Key Cholinergic and Adrenergic Drugs

front 1

Drug: Hemicholinium

(Cholinergic)

back 1

Class: Inhibitor of ACh synthesis (blocks choline uptake)

Clinical Applications: Research tool; not used therapeutically

Common Side Effects: Not clinically used

Serious Adverse Effects: Experimental toxicity

Contraindications: Not applicable (not for clinical use)

Therapeutic Considerations: Blocks high-affinity choline transporter → ↓ ACh synthesis; important in experimental neuropharmacology

front 2

Drug: Vesamicol

(Cholinergic)

back 2

Class: Inhibitor of ACh storage

Clinical Applications: Experimental use only

Common Side Effects: Not used in humans Serious Adverse Effects: Not applicable

Contraindications: N/A

Therapeutic Considerations: Inhibits vesicular ACh transporter (VAChT), preventing ACh from entering synaptic vesicles

front 3

Drug: Botulinum Toxin

(Cholinergic)

back 3

Class: Neurotoxin; inhibits ACh release

Clinical Applications: Dystonia, cosmetic reduction of wrinkles, chronic migraine, hyperhidrosis, strabismus

Common Side Effects: Local muscle weakness, ptosis, flu-like symptoms

Serious Adverse Effects: Dysphagia, respiratory depression if systemically absorbed

Contraindications: Infection at injection site, hypersensitivity

Therapeutic Considerations: Cleaves SNARE proteins needed for vesicle fusion, preventing ACh release; effects are long-lasting but reversible

front 4

Drug: Scopolamine

(Cholinergic)

back 4

Class: Muscarinic receptor antagonist

Clinical Applications: Motion sickness (transdermal), postoperative nausea

Common Side Effects: Dry mouth, drowsiness, blurred vision

Serious Adverse Effects: Hallucinations, confusion (especially in elderly)

Contraindications: Narrow-angle glaucoma

Therapeutic Considerations: Crosses the blood-brain barrier; central effects dominate at therapeutic doses

front 5

Drug: Atropine

(Cholinergic)

back 5

Class: Muscarinic receptor antagonist

Clinical Applications: Bradycardia, organophosphate poisoning, pre-op secretion reduction, pupil dilation for eye exams

Common Side Effects: Dry mouth, tachycardia, photophobia

Serious Adverse Effects: Hyperthermia, delirium, urinary retention

Contraindications: Glaucoma, urinary tract obstruction

Therapeutic Considerations: Non-selective M antagonist; dose-dependent tissue effects (low = salivary/gastric, high = heart and eyes)

front 6

Drug: Ipratropium

(Cholinergic)

back 6

Class: Muscarinic antagonist (inhaled)

Clinical Applications: COPD, asthma (less effective for acute bronchospasm than β2 agonists)

Common Side Effects: Dry mouth, cough

Serious Adverse Effects: Rare systemic effects due to poor absorption

Contraindications: Hypersensitivity to atropine derivatives or soy/peanut (formulation dependent)

Therapeutic Considerations: Quaternary amine → minimal CNS effects; short-acting bronchodilator

front 7

Drug: Tiotropium

(Cholinergic)

back 7

Class: Long-acting muscarinic antagonist (LAMA)

Clinical Applications: Maintenance therapy for COPD, sometimes used in asthma

Common Side Effects: Dry mouth, constipation, urinary retention

Serious Adverse Effects: Paradoxical bronchospasm, atrial fibrillation (rare)

Contraindications: Hypersensitivity to tiotropium or lactose (inhaler formulation)

Therapeutic Considerations: Longer duration than ipratropium; once-daily dosing improves adherence

front 8

Drug: Solifenacin

(Cholinergic)

back 8

Class: Muscarinic M3 receptor antagonist

Clinical Applications: Overactive bladder, urinary urgency/incontinence

Common Side Effects: Dry mouth, constipation, blurred vision

Serious Adverse Effects: Urinary retention, QT prolongation (rare)

Contraindications: Urinary retention, gastric retention, uncontrolled narrow-angle glaucoma

Therapeutic Considerations: Higher selectivity for M3 → fewer CNS effects vs. older antimuscarinics

front 9

Drug: Tolterodine

(Cholinergic)

back 9

Class: Muscarinic antagonist (M3 receptor antagonist)

Clinical Applications: Overactive bladder symptoms

Common Side Effects: Dry mouth, constipation, headache

Serious Adverse Effects: QT prolongation, confusion (especially in elderly)

Contraindications: Urinary/gastric retention, narrow-angle glaucoma

Therapeutic Considerations: Less M3 selectivity than solifenacin; caution in elderly patients

front 10

Drug: Bethanechol

(Cholinergic)

back 10

Class: Muscarinic receptor agonist

Clinical Applications: Urinary retention, postoperative ileus

Common Side Effects: Diarrhea, salivation, abdominal cramps

Serious Adverse Effects: Bronchospasm, hypotension, bradycardia

Contraindications: Asthma, GI obstruction, peptic ulcer, bradycardia

Therapeutic Considerations: Selective for muscarinic receptors; does not cross BBB

front 11

Drug: Nicotine

(Cholinergic)

back 11

Class: Nicotinic receptor agonist

Clinical Applications: Smoking cessation (patches, gums), experimental studies on ganglionic stimulation

Common Side Effects: Nausea, dizziness, headache

Serious Adverse Effects: Arrhythmias, seizures at high doses

Contraindications: Hypersensitivity, caution in cardiovascular disease

Therapeutic Considerations: Stimulates both sympathetic and parasympathetic ganglia; high doses cause receptor desensitization

front 12

Drug: Edrophonium

(Cholinergic)

back 12

Class: Short-acting acetylcholinesterase inhibitor

Clinical Applications: Diagnosis of myasthenia gravis (Tensilon test)

Common Side Effects: Increased salivation, GI cramping

Serious Adverse Effects: Bradycardia, bronchospasm

Contraindications: Intestinal or urinary obstruction

Therapeutic Considerations: Rapid onset and short duration; does not cross Blood Brain Barrier

front 13

Drug: Neostigmine

(Cholinergic)

back 13

Class: Reversible acetylcholinesterase inhibitor

Clinical Applications: Myasthenia gravis, reversal of neuromuscular blockade, urinary retention

Common Side Effects: Nausea, diarrhea, bradycardia

Serious Adverse Effects: Cholinergic crisis, bronchospasm

Contraindications: Peritonitis, mechanical obstruction

Therapeutic Considerations: Quaternary compound (does not cross BBB); longer duration than edrophonium

front 14

Drug: Physostigmine

(Cholinergic)

back 14

Class: Reversible acetylcholinesterase inhibitor

Clinical Applications: Antidote for anticholinergic toxicity (e.g., atropine overdose)

Common Side Effects: Sweating, nausea, bradycardia

Serious Adverse Effects: Seizures, cholinergic crisis

Contraindications: Asthma, cardiovascular disease

Therapeutic Considerations: Tertiary amine; crosses BBB, unlike neostigmine

front 15

Drug: Donepezil

(Cholinergic)

back 15

Class: Centrally acting acetylcholinesterase inhibitor

Clinical Applications: Alzheimer’s disease (mild to moderate)

Common Side Effects: Nausea, diarrhea, insomnia

Serious Adverse Effects: Bradycardia, syncope

Contraindications: Hypersensitivity

Therapeutic Considerations: Long half-life allows once-daily dosing; selectively enhances central cholinergic transmission

front 16

Drug: Methacholine

(Cholinergic)

back 16

Class: Muscarinic receptor agonist

Clinical Applications: Diagnosis of bronchial hyperreactivity (asthma test)

Common Side Effects: Coughing, chest tightness

Serious Adverse Effects: Bronchospasm, hypotension

Contraindications: Severe asthma, cardiovascular disease

Therapeutic Considerations: Inhaled; used under medical supervision only; highly sensitive test for asthma diagnosis

front 17

Drug: Succinylcholine

(Cholinergic)

back 17

Class: Depolarizing neuromuscular blocker

Clinical Applications: Muscle relaxation during intubation and surgery

Common Side Effects: Muscle fasciculations, postoperative myalgia

Serious Adverse Effects: Malignant hyperthermia, hyperkalemia, apnea

Contraindications: History of malignant hyperthermia, burns, neuromuscular disease

Therapeutic Considerations: Rapid onset, short duration; metabolized by plasma cholinesterases

front 18

Drug: Pancuronium

(Cholinergic)

back 18

Class: Non-depolarizing neuromuscular blocker

Clinical Applications: Adjunct to anesthesia for muscle paralysis

Common Side Effects: Tachycardia, hypotension

Serious Adverse Effects: Prolonged paralysis, anaphylaxis

Contraindications: Hypersensitivity, caution in renal/hepatic impairment

Therapeutic Considerations: Long-acting agent; reversed by cholinesterase inhibitors (e.g., neostigmine)

front 19

Drug: Tubocurarine

(Cholinergic)

back 19

Class: Non-depolarizing neuromuscular blocker

Clinical Applications: Historical use in anesthesia for muscle relaxation

Common Side Effects: Hypotension (histamine release), prolonged weakness

Serious Adverse Effects: Respiratory paralysis

Contraindications: Asthma, hypotension, myasthenia gravis

Therapeutic Considerations: Rarely used today; replaced by safer non-depolarizing agents

front 20

Drug: Methyltyrosine

(Adrenergic)

back 20

Class: Tyrosine hydroxylase inhibitor

Clinical Applications: Treatment of pheochromocytoma (rare adrenal tumor)

Common Side Effects: Sedation, diarrhea, anxiety

Serious Adverse Effects: Extrapyramidal symptoms, hypotension

Contraindications: Hypersensitivity, Parkinson’s disease

Therapeutic Considerations: Depletes catecholamine synthesis; used adjunctively before surgery in pheochromocytoma

front 21

Drug: Reserpine

(Adrenergic)

back 21

Class: VMAT (vesicular monoamine transporter) inhibitor

Clinical Applications: Rarely used now; previously used for hypertension

Common Side Effects: Nasal congestion, GI upset, sedation

Serious Adverse Effects: Depression, suicidal ideation (due to CNS catecholamine depletion)

Contraindications: History of depression, peptic ulcer

Therapeutic Considerations: Depletes NE, dopamine, serotonin in both CNS and PNS; long-lasting effects

front 22

Drug: Guanethidine

(Adrenergic)

back 22

Class: Adrenergic neuron blocker

Clinical Applications: Rarely used antihypertensive

Common Side Effects: Orthostatic hypotension, diarrhea, sexual dysfunction

Serious Adverse Effects: Bradycardia, fluid retention

Contraindications: MAOI therapy, pheochromocytoma

Therapeutic Considerations: Replaces NE in nerve terminals and inhibits NE release; slow onset of action

front 23

Drug: Midodrine

(Adrenergic)

back 23

Class: Alpha-1 agonist (prodrug)

Clinical Applications: Orthostatic hypotension Common

Side Effects: Paresthesia, piloerection, urinary retention

Serious Adverse Effects: Supine hypertension

Contraindications: Severe heart disease, urinary retention

Therapeutic Considerations: Converted to active form (desglymidodrine); avoid dosing near bedtime to prevent nocturnal hypertension

front 24

Drug: Clonidine

(Adrenergic)

back 24

Class: Alpha-2 adrenergic receptor agonist

Clinical Applications: Hypertension, ADHD, withdrawal symptoms

Common Side Effects: Dry mouth, sedation, dizziness

Serious Adverse Effects: Rebound hypertension on sudden withdrawal

Contraindications: Bradyarrhythmia, severe coronary insufficiency

Therapeutic Considerations: Decreases sympathetic outflow from CNS; taper gradually to avoid rebound hypertension

front 25

Drug: Dobutamine

(Adrenergic)

back 25

Class: Beta-1 adrenergic receptor agonist

Clinical Applications: Acute heart failure, cardiogenic shock

Common Side Effects: Tachycardia, hypertension, palpitations

Serious Adverse Effects: Arrhythmias

Contraindications: Idiopathic hypertrophic subaortic stenosis

Therapeutic Considerations: Increases contractility and output more than heart rate; short-term IV use only

front 26

Drug: Albuterol

(Adrenergic)

back 26

Class: Beta-2 adrenergic receptor agonist

Clinical Applications: Acute bronchospasm (asthma, COPD), bronchodilator

Common Side Effects: Tremor, nervousness, tachycardia

Serious Adverse Effects: Paradoxical bronchospasm, arrhythmias

Contraindications: Hypersensitivity to albuterol or excipients

Therapeutic Considerations: Rapid onset, short-acting; overuse may cause receptor desensitization

front 27

Drug: Amphetamine

(Adrenergic)

back 27

Class: Indirect-acting sympathomimetic

Clinical Applications: ADHD, narcolepsy

Common Side Effects: Insomnia, anorexia, increased BP

Serious Adverse Effects: Dependence, psychosis, cardiovascular events

Contraindications: Cardiovascular disease, hypertension, hyperthyroidism

Therapeutic Considerations: Increases release of NE and dopamine from nerve terminals; CNS stimulant

front 28

Drug: Pseudoephedrine

(Adrenergic)

back 28

Class: Mixed-acting sympathomimetic

Clinical Applications: Nasal congestion

Common Side Effects: Insomnia, anxiety, hypertension

Serious Adverse Effects: Tachycardia, stroke (rare)

Contraindications: Severe hypertension, MAOI use

Therapeutic Considerations: Direct agonist at α and β receptors and promotes NE release; less CNS stimulation than amphetamines

front 29

Drug: Phenylephrine

(Adrenergic)

back 29

Class: Alpha-1 adrenergic receptor agonist

Clinical Applications: Nasal congestion, hypotension, pupil dilation

Common Side Effects: Hypertension, reflex bradycardia

Serious Adverse Effects: Arrhythmias, rebound congestion (nasal)

Contraindications: Severe hypertension, ventricular tachycardia

Therapeutic Considerations: Used topically or IV; avoid prolonged use in nasal sprays to prevent rebound effect

front 30

Drug: Tyramine

(Adrenergic)

back 30

Class: Indirect sympathomimetic (naturally occurring amine)

Clinical Applications: No therapeutic use; relevance in food-drug interactions

Common Side Effects: None under normal metabolism

Serious Adverse Effects: Hypertensive crisis (with MAOIs)

Contraindications: Use with MAO inhibitors

Therapeutic Considerations: Found in fermented foods; releases NE from adrenergic terminals; degraded by MAO under normal conditions

front 31

Drug: Cocaine

(Adrenergic)

back 31

Class: Monoamine reuptake inhibitor

Clinical Applications: Local anesthesia (ENT procedures); vasoconstriction

Common Side Effects: Euphoria, tachycardia, insomnia

Serious Adverse Effects: Seizures, arrhythmias, myocardial infarction

Contraindications: Cardiovascular disease, concurrent sympathomimetic use

Therapeutic Considerations: Inhibits reuptake of NE, dopamine, serotonin; significant abuse potential and toxicity. It increases sympathetic activity

front 32

Drug: Phentolamine

(Adrenergic)

back 32

Class: Non-selective alpha-adrenergic receptor antagonist

Clinical Applications: Pheochromocytoma (diagnosis and management), hypertensive emergencies due to catecholamines

Common Side Effects: Hypotension, reflex tachycardia

Serious Adverse Effects: Arrhythmias, myocardial ischemia

Contraindications: Coronary artery disease

Therapeutic Considerations: Short-acting; used in surgery or catecholamine excess

front 33

Drug: Prazosin

(Adrenergic)

back 33

Class: Selective alpha-1 adrenergic receptor antagonist

Clinical Applications: Hypertension, benign prostatic hyperplasia (BPH)

Common Side Effects: Dizziness, orthostatic hypotension, headache

Serious Adverse Effects: Syncope (especially first dose)

Contraindications: Hypersensitivity

Therapeutic Considerations: “First-dose effect” — start with low dose at bedtime

front 34

Drug: Tamsulosin

(Adrenergic)

back 34

Class: Alpha-1A adrenergic receptor antagonist

Clinical Applications: BPH (urinary retention)

Common Side Effects: Dizziness, abnormal ejaculation

Serious Adverse Effects: Hypotension (less than with prazosin)

Contraindications: Known hypersensitivity

Therapeutic Considerations: Selective for prostate/bladder neck; minimal BP effects

front 35

Drug: Labetalol & Carvedilol

(Adrenergic)

back 35

Class: Mixed alpha-1 and beta adrenergic receptor antagonists

Clinical Applications: Hypertensive emergencies (labetalol), heart failure and hypertension (carvedilol)

Common Side Effects: Fatigue, dizziness, orthostatic hypotension

Serious Adverse Effects: Bradycardia, bronchospasm

Contraindications: Asthma, AV block, bradycardia

Therapeutic Considerations: Dual blockade reduces BP without reflex tachycardia; carvedilol has antioxidant properties

front 36

Drug: Propranolol

(Adrenergic)

back 36

Class: Non-selective beta adrenergic receptor antagonist

Clinical Applications: Hypertension, angina, arrhythmias, migraine prophylaxis

Common Side Effects: Fatigue, cold extremities, bradycardia

Serious Adverse Effects: Bronchospasm, depression, heart block

Contraindications: Asthma, severe bradycardia

Therapeutic Considerations: Crosses BBB; not selective, affects β1 and β2 equally

front 37

Drug: Atenolol

(Adrenergic)

back 37

Class: Beta-1 selective adrenergic receptor antagonist

Clinical Applications: Hypertension, angina, post-MI

Common Side Effects: Fatigue, dizziness

Serious Adverse Effects: Bradycardia, AV block

Contraindications: Sinus bradycardia, AV block

Therapeutic Considerations: Less CNS penetration than propranolol; preferred in patients with asthma or COPD