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65 Cards in this Set
- Front
- Back
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Phenylephrine |
(Neo-Synephrine) - Decongestant α1 Adrenergic Agonist - Increased vasoconstriction --- increased systolic and diastolic pressures |
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Methoxamine |
(Vasoxyl) α1 Adrenergic Agonist - Increased vasoconstriction --- increased systolic and diastolic pressures |
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Oxymetazoline |
(Dristan) - Decongestant α1 Adrenergic Agonist - Increased vasoconstriction --- increased systolic and diastolic pressures |
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Tetrahydrozoline |
(Visine) - Used for eye redness α1 Adrenergic Agonist - Increased vasoconstriction --- increased systolic and diastolic pressures |
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Clonidine |
(Catapres) - treat hypertension α2 Adrenergic Agonists - decreased sympathetic tone (decrease NE release from presynaptic terminal via auto-inhibitory receptors), hypotension - peripheral vasoconstriction (postsynaptic) - Like the NE blockade drugs |
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Xylazine |
(Rompun) - analgesia and sedation α2 Adrenergic Agonists - decreased sympathetic tone (decrease NE release from presynaptic terminal), hypotension - peripheral vasoconstriction (postsynaptic) |
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Dobutamine |
(Dobutrex) - short term treatment of heart failure β1 Adrenergic Agonist - Increase force of heart contraction, more than rate (so not more O2 required) |
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Isoproterenol |
(Isuprel) - heart failure (β1), asthma (β2) Nonselective β Adrenergic Agonist - β1 - cardiac stimulatory effects - β2 - bronchodilation effects |
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Albuterol Terbutaline Metaproterenol |
(Salbutamol, Bricanyl, ??) - Bronchodilator β2 Adrenergic Agonist - β1 effects increased at higher doses - Bronchodilation - Prevents premature labor |
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BRL 37344 BMS - |
β3 Adrenergic Agonists - Found in adipose tissue - Increases lipolysis - Being explored for treatment of obesity |
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Tyramine |
Indirectly Acting Sympathomimetic - **Transported** into nerve terminal, increase NE release - Found in cheese and wine - **No reuptake in adrenal (no transporter), so no increase in Epinephrine release** |
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Amphetamines
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Indirectly Acting Sympathomimetic - **Transported** into nerve terminal, increase NE release - Powerful CNS stimulant - euphoria, psychosis, arousal - **No reuptake in adrenal (no transporter), so no increase in Epinephrine release** |
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Cocaine
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Norepinephrine Reuptake Blocker - Increased NE in synaptic cleft - Vasoconstrictive - Mood altering CNS affects
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Imipramine Amitryptyline |
Norepinephrine Reuptake Blocker - Increased NE in synaptic cleft - Tricyclic antidepressants - modulate NE reuptake in the CNS |
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Ephredrine |
Mixed Acting Sympathomimetics - Cause release of catecholamines by going into the synaptic cleft and binding receptors and go into the terminal via a transporter and cause increase release of NE. - Increased blood pressure, bladder sphincter tone, bronchodilation - Not degraded by MAO or COMT - long acting |
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Pseudoephedrine |
(Sudafed) - Mixed Acting Sympathomimetics - Cause release of catecholamines by going into the synaptic cleft and binding receptors and go into the terminal via a transporter and cause increase release of NE. - Low CV and CNS effects - isomer of methamphetamines |
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Guanethidine |
Blocks NE release - anti-hypertensive activity - Taken up via a transporter, accumulated in vesicles and replaces NE, is released into cleft, has no activity - Doesn't affect adrenal (no transporters), doesn't cross BBB (no CNS effects) |
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Bretylium |
Blocks NE release - anti-hypertensive activity - Taken up via a transporter, prevents NE release by decreasing nerve excitability. - Doesn't affect adrenal (no transporters), doesn't cross BBB (no CNS effects) |
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Reserpine |
NE Vesicular Storage Blocker - Prevents accumulation of NE in vesicles, basically releasing empty vesicles into cleft. - Can get in across plasma membrane without a transporter, so can affect the adrenal release of epinephrine!! - Research tool, used for hypertension |
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α-methyl-DOPA |
False transmitter release - Taken up into nerve terminal, converted to α-methyl-NE, released in vesicles instead of NE, low activity - Antihypertensive |
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α-CH3-p-tyrosine |
NE synthesis inhibitor - Blocks tyrosine hydroxylase |
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Norepinephrine effect on NE release? |
Inhibits production, feedback inhibition, by competing for Tyrosine hydroxylase cofactors |
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Disulfiram |
(antabuse) - anti-alcohol drug Inhibits NE synthesis Blocks dopamine-β-hydroxylase |
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Pargyline Moclobemide |
Monamine Oxidase Inhibitor - Antidepressent - More NE in vesicles - Cheese syndrome (don't want to have tyramine to release NE because there is so much more NE in those vesicles) |
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Tolcapone |
COMT Inhibition - Not much therapeutic action |
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Dibenamine Phenoxybenzamine |
Irreversible α Receptor Blockers - alkylates receptors, lasts days. - treats hypertension - Need to make new receptors to overcome effects |
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Phentolamine |
Reversible α Receptor Blocker - short-acting (hours) - Treats hypertension - Can cause tachycardia, increase NE release from blocking presynaptic α2 (inhibitor pathway) |
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Prazosin |
Selective α1 blocker - Decreases vascular tone, no effect on the presynaptic α2 inhibitory pathway) - Used for hypertension, less tachycardia |
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Tamsulosin |
(Flomax) Selective α1A blocker - Improves urination in men with benign prostatic hyperplasia. Not used for hypertension. |
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Yohimbine |
Selective α2 blocker - Increases NE release, blocks inhibitory presynaptic receptors. - Not used in ppl. - This can be used to reverse sedation of α2 agonists (like Xylazine) |
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Side Effects of α Receptor Blockers |
- Postural hypotension (venous pooling) - Reflexive tachycardia - Nasal stuffiness - Increased gastrointestinal motility |
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Therapeutic Uses of α Receptor Blockers |
- Hypertension - Congestive heart failure - Peripheral vascular disease - Benign Prostatic hyperplasia - Shock |
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Therapeutic uses of β Receptor Blockers |
- Cardiac arrythmias - Hypertension (decrease cardiac output) - Prophylactic - Anxiolytic - Glaucoma (decrease production of aqueous humor) |
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Propranolol Pindolol Timolol |
Non-selective β-Blocker - Decrease heart rate, contractility, output - Significant withdrawal in Propranolol (upregulation of receptors) - Pindolol and Timolol have less membrane stabilization - Timolol used for glaucoma |
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Metoprolol |
Selective β1 Blocker - Cardioselective |
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Butoxamine |
Selective β2 Blocker - Selective for blocking sooth muscle relaxation and vasodilation without cardiac effects |
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Side Effects of β Receptor Blockers |
- Cardiac failure - Bradycardia - Bronchial asthma - Diabetics using oral hypoglycemics (block β2 mediated hepatic glucose release) |
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Hemicholinium |
- Blocks uptake of choline (which is rate-limiting step of ACh synthesis) into nerve terminal to limit synthesis of Acetylcholine |
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Vesamicol |
Blocks transport of ACh into nerve terminal vesicles, limiting the amount store for release. |
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Botulinus toxin |
- Blocks vesicle fusion at synaptic cleft, not allowing ACh release. - Breaks synaptobrevin - Causes flaccid paralysis leading to death by paralysis of respiratory muscles |
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How is ACh cleared from synaptic terminals? |
Acetylcholinesterase breaks it down (unlike catecholamines that undergo reuptake) |
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Methacholine |
Parasympathomimetic - Selective muscarinic activity - Used for GI and urinary stimulation |
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Carbachol |
Parasympathomimetic - Muscarinic and nicotinic activity - Limited use due to ganglionic stimulation - Used for glaucoma - Not susceptible to cholinesterase |
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Bethanecol |
Parasympathomimetic - Selective muscarinic activity - used to treat urinary retention by stimulating bladder contraction - Not susceptible to cholinesterase |
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Pilocarpine |
Parasympathomimetic - Mainly muscarinic activity - Increases sweating and salivation - Used to counteract mydriasis of atropine - increase BP and tachycardia |
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Arecoline |
Parasympathomimetic - Betel nut! - acts at nicotinic and muscarinic receptors - Increased GI tract peristalsis - worm expulsion (previous use) |
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Muscarine |
Parasympathomimetic - Amanita muscaria - Acts at muscarinic receptors - increased sweating, salivation, lacrimation - bowel evacuation. Cardiovascular collapse. Death. - Antidote = muscarinic receptor antagonist = atropine. |
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Atropine Homoatropine (less potent) |
Antimuscarinic agent - High affinity muscarinic antagonist (non-selective - hits all muscarinic) - Causes tachycardia, drying of airways and dilation, decreased GI motility - Preanesthetic, anti asthmatic |
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Scopolamine |
Antimuscarinic agent - Preanesthetic, decreases motion sickness - Sedates mentally ill patients |
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Propantheline |
Synthetic antimuscarinic agent - No CNS effects (low dose) - Mitigates GI spasm and diarrhea - Prepare for rectal exams on horses |
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Tropicamide |
Synthetic antimuscarinic agent - Induce mydriasis - used at eye doctor - Short acting - preferred over atropine - Quick recovery from cycloplegia (paralysis of accommodation) |
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Narrow acute glaucoma tx |
- Caused by big iris blocking drainage of humor, use muscarinic agonists to induce miosis (parasympathetic) - Pilocarpine, physostigmine used to allow drainage, reduce pressure until surgery |
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Wide angle glaucoma tx |
- beta antagonist timolol decrease aqueous humor production - Long lasting anti-AChE drugs used - Surgery not helpful |
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Nicotine |
Nicotinic agent - ganglionic stimulant (para- and sympathetic effects) - CNS effects - No therapeutic uses - Stimulates adrenal medulla - increased EPI, NE |
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Lobeline DMPP TMA |
Nicotinic Agents - ganglionic stimulants |
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Hexamethonium |
Nicotinic Ganglionic Blocker |
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Trimethaphan |
Nicotinic Ganglionic Blocker - Used in vet med to lower BP during surgery |
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Edrophonium |
Anti-AChE (reversible) (Tensilon) - Diagnoses Myasthenia Gravis - Short Acting - Binds on AChE |
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Physostigmine |
Anti-AChE (carbamylation) - Slowly reversible, crosses BBB - Treats glaucoma - Tx for atropine poisoning |
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Neostigmine |
Anti-AChE (carbamylation) - Does not cross BBB - Used to treat myasthenia gravis |
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Pyridostigmine |
Anti-AChE (carbamylation) - shorter half life than neostigmine and physostigmine - used by soldiers expecting nerve gas exposure |
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Nerve Gases Sarin VX Gas |
Anti-AChE (phosphorylation, irreversible) - enzyme replenishment takes WEEKS |
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Neuromuscular Blocker Therapeutic Uses |
- Facilitate endotracheal intubation - Facilitate surgery w/ less anesthesia - Orthopedic surgeries with fracture alignment - Electroshock psychiatric txs
NEED MECHANICAL VENTILATION |
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d-Turbocurarine Pancuronium Atracurium |
Non-depolarizing competitive neuromuscular blockers - Can be overcome by increasing [ACh] - Do not affect smooth or cardiac muscle |
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Succinylcholine |
Depolarizing neuromuscular blocker - Non-competitive antagonist - Desensitizes ACh receptors - causes some activation first. - Hydrolyzed by plasma cholinesterases - Really short onset time and duration |
