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66 Cards in this Set
- Front
- Back
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Methacholine
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Muscarinic Receptor Agonist
Used in diagnosis of asthma (Methacholine challenge test – leads to bronchiole hyper-responsiveness in asthmatics) |
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Carbachol
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Muscarinic Receptor Agonist
Used topically as a mitotic agent to treat Glaucoma - Affinity for Nm receptor - Resistant to Cholinesterase |
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Bethanecol
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Muscarinic Receptor Agonist
Used to increase GIT and urinary tract motility |
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Pilocarpine
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Muscarinic Receptor Agonist
Used topically as a mitotic in Glaucoma Used as a sialogogue to increase saliva secretion |
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Atropine
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Muscarinic Receptor Antagonist
Pupil dilation, Tachycardia, Decreased secretions (salivary, bronchial and GIT) 1. Produce mydriasis for ophthalmological examination 2. Reverse sinus bradycardia caused by excessive vagal tone 3. Inhibit excessive salivation and mucus secretion during anaesthesia and surgery (intubation) 4. Counteract the effects of muscarine poisoning and poisoning with anticholinesterases |
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Scopolamine
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Muscarinic Receptor Antagonist
To prevent motion sickness |
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Pirenzepine
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Muscarinic Receptor Antagonist
Treatment of peptic ulcers |
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Ipratropium
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Muscarinic Receptor Antagonist
Used in chronic obstructive pulmonary disease (COPD) - Reduces bronchial secretions Used in asthma - Bronchoconstrictive component is mediated by increased cholinergic neural tone |
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Hemicholinium
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Prevents Choline re-uptake
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Vesamicol
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Prevents vesicular storage of Ach
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Botulinium Toxin
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Used in cases with increased skeletal muscle tone, Lower esophageal sphincter tone, Focal dystonia’s
Degrades synaptobrevin (SNARE) and prevents vesicle fusion/exocytosis |
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AChE inhibitors
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Elevates the synaptic concentration of Ach – Parasympathomimetic
1. Used to increase neuromuscular transmission (skeletal) 2. Used to increase parasympathetic tone 3. Used to increase central cholinergic neurotransmission 4. Used in reversal of paralysis from non-depolarizing neuromuscular blockers 5. Used in reversal of anti-cholinergic poisoning |
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Edrophonium
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AchE Inhibitors
(Anticholinesterase) Simple alcohol Used for diagnosis Myasthenia Gravis and Eaton Lambert Short duration |
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Neostigmine, Physostigmine
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AchE Inhibitors
(Anticholinesterase) Carbamic acid derivative Useful for treating Myasthenia Gravis Reversal of neuromuscular blockers Longer duration |
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Organophosphates
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AchE Inhibitors
(Anticholinesterase) Used in flea/tick medication - Irreversible - Toxic |
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Succinylcholine
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Nicotinic Receptor Agonists (Depolarizing neuromuscular blocker)
Used for short term paralysis (during intubation) - Short duration as metabolized by psuedocholinesterase (BuChE) Depolarizing neuromuscular blocker - Excessive activation of Nm receptor leading to muscle fasciculation - Eventual desensitization of Nm receptor leading to muscle paralysis SE: Bradykardia (M2) K+ release Prolonged paralysis Malignant hyperthermia |
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Pancuronium
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Nicotinic Receptor Antagonist (Non-Depolarizing neuromuscular blocker)
- Derived from D-tubocurarine - Long lasting |
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Vecuronium
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Nicotinic Receptor Antagonist (Non-Depolarizing neuromuscular blocker)
- Derived from D-tubocurarine - Intermediate |
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Mivacurium
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Nicotinic Receptor Antagonist (Non-Depolarizing neuromuscular blocker)
- Derived from D-tubocurarine - Short acting |
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Methoxamine
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α1 Adrenergic Receptor Agonist
Limited use except for hypotension from circulatory shock SE: Reflex vagal sinus bradycardia |
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Phenylephrine
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α1 Adrenergic Receptor Agonist
Used as nasal decongestant SE: Unwanted hypertension |
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Prazosin
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α1 Adrenergic Receptor Antagonist
Used for treatment of hypertension and Benign Prostatic Hypertrophy SE: Postural / Orthostatic Hypotension related to 1st dose |
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Tamsulosin
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α1 Adrenergic Receptor Antagonist
Used for Benign Prostatic Hypertension (increased rate and frequency of urination) – allows proper filling of the bladder before urination - More selective for genitourinary smooth muscle receptor subtype α1A SE: Less postural / orthostatic hypotension |
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Clonidine
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α2 Adrenergic Receptor Agonist
Used for treatment of hypertension (decreased peripheral sympathetic outflow) and opioid withdrawal SE: Bradycardia Hypotension |
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Yohimbine
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α2 Adrenergic Receptor Antagonist
Previously used for male impotence SE: Bradycardia Hypertension |
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Isoproterenol
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Non Selective β Adrenergic Receptor Agonist
Used for emergency arrhythmias and bronchospasm More selective agonist now available SE: Hypertension Palpitations Tremor |
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Dobutamine
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Selective β1 Adrenergic Receptor Agonist
Used in the ACUTE management of heart failure - Has prominent inotropic effects resulting in increased contractility and cardiac output - Short half life due to COMT metabolism |
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Albuterol
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Selective β2 Adrenergic Receptor Agonist
Used as ‘asthma reliever’ - Rapid action (15 min) - Short duration (4-6 hours) |
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Salmeterol
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Selective β2 Adrenergic Receptor Agonist
Used for treatment of asthma (prevention of bronchoconstriction) (long acting beta agonist – LABA’s) Due to long lipophilic side chains that resist degradation - Enhance duration (12-24 hours) |
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Propranolol
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Non Selective β Adrenergic Receptor Antagonist
Used for hypertension and angina SE: Sedation (central effect) Dyspnea |
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Timolol
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Non Selective β Adrenergic Receptor Antagonist
Ocular formulation used in treatment of glaucoma (reduced production of aqueous humor) |
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Esmolol
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Selective β1 Adrenergic Receptor Antagonist
Used in emergency β receptor blockade as in a thyroid storm (half life = 4 min) |
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Atenolol
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Selective β1 Adrenergic Receptor Antagonist
Used in treatment of hypertension and angina Improves life expectance in patients with heart failure Clinical benefit in heart failure through volume reduction (decrease afterload) via decrease in renin production and vasodilation (decrease preload) Contraindication in severe heart failure |
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Acebutolol
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Partial β1 Adrenergic Receptor Agonist
Used for treatment of hypertension in patients with bradycardia or low cardiac reserve |
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Carvedilol
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Non Selective β and α1 Antagonist
α1 blockade results in vasodilation β1 blockade prevents a reflex sympathetic increase in heart rate Combine to decrease blood pressure Also used in treatment of heart failure Clinical benefit in heart failure through volume reduction (decrease afterload) via decrease in renin production and vasodilation (decrease preload) Contraindication in severe heart failure |
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Cocaine
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Inhibitors of Catecholamine Re-uptake
Inhibits NET |
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Tricyclic Antidepressants (TCA’s)
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Inhibitors of Catecholamine Re-uptake
Inhibits NET |
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Impiramine
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Inhibitors of Catecholamine Re-uptake
Used for treating mild depression SE: Postural hypotension Tachycardia |
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Reserpine
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Inhibitors of Catecholamine Storage
Blocks VMAT |
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Tyramine
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Inhibitors of Catecholamine Storage
Transported via VMAT and displaces vesicular NE |
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MAO inhibitors
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Inhibitors of Catecholamine Metabolism
Used for treatment of mild depression |
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Phenelzine
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Inhibitors of Catecholamine Metabolism
Non selective MAO inhibitor Implicated in elevated tyramine leading to hypertensive crisis |
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Selegiline
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Inhibitors of Catecholamine Metabolism
Selective MAO B inhibitor Safe with respect to dietary restriction Also useful for Parkinson’s |
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Amphetamines
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Inhibitors of Re-uptake and Storage
- Displaces endogenous catecholamines from storage vesicles - Blocks NET - Weak inhibitor of MAO |
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Methylphenidate
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Inhibitors of Re-uptake and Storage
Used for ADHA |
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Pseudoephridine
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Inhibitors of Re-uptake and Storage
Used for nasal decongestion |
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Selective β2 Adrenergic Receptor Agonist
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relaxation of vascular, bronchial, and gastrointestinal smooth muscle
- Used for treatment of Asthma - Pulmonary drug delivery enhances selectivity of β2 adrenergic receptor agonist, avoids cardiac (β1) and skeletal (β2) side effects |
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Parasympathetic pre-ganglionic neurotransmitters
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Acetylcholine (nicotinic)
Enkephalin, Substance P, GnRH |
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Parasympathetic post-ganglionic neurotransmitters
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Acetylcholine (muscarinic)
VIP |
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Sympathetic pre-ganglionic neurotransmitters
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Acetylcholine (nicotinic)
Enkephalin, Substance P, GnRH |
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Sympathetic post-ganglionic neurotransmitters
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Norepinephrine (adrenergic)
Neuropeptide Y, ATP |
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M1 Receptors
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Increase IP3/DAG
Increase calcium and PKC Stimulate parietal cells Increase gastric acid secretion |
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M2 Receptors
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Decrease cAMP
Increase potassium channel opening leading to hyperpolarization Inhibit cardiac muscle Decrease HR and conduction velocity |
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M3 Receptors
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Increase IP3/DAG
Increase calcium and PKC Smooth muscle contraction Vasodilation (NO) |
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Muscarinic Receptor Agonist
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Eye:
- Pupillary constriction - Outflow of aqueous humor leads to a decrease in intraocular pressure - Benefits Glaucoma GIT, Bladder, Urinary tract: - Contract smooth muscle - Increase motility - Restore GIT and UT motility after anaesthesia or surgery Salivary glands: - Increase salivation - Benefits xerostomia |
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Muscarinic Receptor Antagonist
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Action:
- Bind to muscarinic receptors and prevent Ach from exerting its effects *Competitive Antagonist |
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Nicotinic Receptor Agonists
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Depolarizing neuromuscular blocker
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Nicotinic Receptor Antagonist
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Non-Depolarizing neuromuscular blocker
Use: - To paralyze skeletal muscles during surgery (more selective on Nm than Nn receptors) Action: - Occupy Nm receptors on skeletal muscle - Have no intrinsic activity - Prevent action of Ach - Muscle cannot contract - Leads to Flaccid paralysis *Competitive Antagonist - Effect can be overcome by increasing Ach levels - Reversal achieved by Ach Esterase Inhibitor |
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α1 Receptor
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Increase IP3/DAG
Increase calcium and PKC Vascular smooth muscle contraction Genitourinary smooth muscle contraction |
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α2 Receptor
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Decrease cAMP
Increase potassium Decrease calcium Decrease norepinephrine release |
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β1 Receptor
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Increase cAMP
Increase PKA Increase Chronotropy and inotropy Increase AV node condution velocity (Stimulation of β1 receptor causes an increase in heart rate and the force of contraction, resulting in increased cardiac output) Also increase Renin secretion from kindeys leading to an increase in blood volume |
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β2 Receptor
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Increase cAMP
Increase PKA Smooth muscle relaxation (Stimulation of β2 receptor causes relaxation of vascular, bronchial, and gastrointestinal smooth muscle) |
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Epinephrine
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Higher affinity for β Receptor
At higher concentrations it has an effect on α1 Receptors At high doses effective at treating anaphylaxis and used for vasoconstriction in conjuctin with local anaesthetic |
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Norepinephrine
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Has affinity for α1 and β1 Receptors
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MAO A
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Converts serotonin to NE to Dopamine and Tyramine
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MAO B
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Converts Dopamine to Serotonin to NE
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