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66 Cards in this Set
- Front
- Back
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A muscarinic agonist that is non-specific and short-lived. Used in glaucoma tx to open the Canal of Schlemm.
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Acetylcholine
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A more specific muscarinic agonist that is rarely used.
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Methacholine
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A non-specific muscarinic agonist that through the addition of an amide is cholinesterase resistant. Treats glaucoma.
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Carbachol
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A tertiary amine M1 agonist used in the tx of glaucoma with profound diaphoretic (sweating) effects.
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Pilocarpine
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A muscarinic specific agonist that is cholinesterase resistant used to Tx GI stasis and urinary stasis (as in post-op and post-partum nonobstructive urinary retention) in the absence of an obstruction.
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Bethanochol
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You should not prescribe Bethanochol if your patient has the following conditions:
Why? |
Hyperthyroidism, peptic ulcer, asthma, bradycardia, heart defects/disease, GI obstructions
Muscarinic Agonist that stimulates PNS |
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Indirect muscarinic agonists function by inhibiting:
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Acetylcholine Esterase
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An indirect muscarinic agonist that causes reversible inhibition of cholinesterase and is used to treat myasthenia gravis, reversal of neuromuscular junction blockade, prevention of post-op distention/urinary retention, and glaucoma.
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Neostigmine
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An indirect muscarinic agonist that is a reversible inhibitor of AchE (binds ionic site) and is used in diagnosis of myasthenia gravis
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Edrophonium Chloride
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An indirect muscarinic agonist that is a tertiary amine similar to neostigmine with CNS effects used in the reversal of centrally active muscarinic antagonists (diazepam)
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Physostigmine
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An indirect muscarinic agonist that is an organophosphate and irreversible inhibitor of AchE used to treat resistant glaucomas.
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Isoflurophate
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A muscarinic antagonist that acts directly on M2/M3 to reduce secretions during anesthesia, management of diarrhea, lowering of HR (low doses) or raising Hr (high doses), and treatment of AchE-I overdose.
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Atropine
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What do cardiologists typically use to treat excessive vagal tone, reduce reflex bradycardia, but has side effects consistent with PNS inhibition?
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Atropine
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A muscarinic antagonist that antagonizes bronchial muscarinic receptors for the treatment of COPD, emphysema, rhinitis and chronic bronchitis:
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Ipratropium Br
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A muscarinic antagonist that is similar to atropine and used in the treatment of Peptic Ulcer Disease (decreases GI PNS stimulation) and is NEVER given with obstructive GI/GU syndromes.
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Propantheline Br
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A muscarinic antagonist that was once used as an obstetric anesthetic that now is used to prevent motion sickness.
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Scopolamine
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An anti-M1 muscarinic antagonist for the intramural ganglia used to inhibit gastic acid secretion but without the cardiac and ocular side effects of atropine.
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Pirenzepine
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A newer muscarinic antagonist that is a selective M3 blocker used to increase warning time of urinary urge in pts with urinary incontinence.
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Darifenacin
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A nicotinic agonist used to aid in smoking cessation and targeting memory in Alzheimer's patients (Vernicidine):
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Nicotine
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When using nicotine gum as smoking cessation therapy, what food products should patients avoid and why?
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Nicotine gum is reliant of alkaline saliva. So, pts should not consume acidic beverages like coffee and cola.
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A nicotinic antagonist similar to trimethaphan and mecamylamine used as autonomic blockers in the tx of HTN and surgical bleeding.
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Hexamethonium
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This class of drugs are used as paralytic agents in intubations, setting broken bones, and delicate surgery:
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Neuromuscular blockers
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A depolarization blocker that functions by overstimulation depolarization that is short-lived (30sec) with fasiculation when given too rapidly.
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Succinylcholine
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A depolarization blocker with a 100-min half life causing histamine release and is renally metabolized. Cannot use with aminoglycosides, ISO, Ca blockers and myasthenia gravis. Reversed with Neostigmine.
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Tubocurare
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A NM blocker with a 10m half-life and mild histamine release. Metabolized by plasma esterase.
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Mivacurium
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A NM blocker with a 50min half-life and some vagal ganglion blockade. Hepatically metabolized.
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Rocuronium
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A NM blocker GABA-mimicking agonist which is is used as an antispastic in spinal cord lesions, multiple sclerosis, and trigeminal neuralgia
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Baclofen
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A NM blocker sedative, hypnotic and anxiolytic medication that enhances GABA binding for joint disease or muscle spasm.
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Diazepam (don't give with EtOH as action amplified)
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An NM blocker that reduces contraction by decreasing Ca2+ levels and is a treatment for Malignant Hyperthermia
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Dantrolene
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Autocoid drug used to treat allergies, motion sickness and nausea and vomiting of pregnancy:
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H1 Antihistamines
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Which cause more sedation:
1st generation antihistimines 2nd generation antihistimines |
1st gen
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Drugs that target H1 receptors are called:
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antihistimines
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Fexofenadine and cetirizine target H1 and are used in what types of reactions?
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Allergic
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Meclizine, Promethazine and Diphenhydramine target H1 and are used for what?
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Anti-emetics (motion sickness, nausea, vertigo)
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Promethazine and Diphenhydramine are best used for what?
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Sedation
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Local anesthetic effects are more effective with which two antihistimines?
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Promethazine and Diphenhydramine
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All second generation antihistimines are indicated for what?
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Allergies
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Which are the two ethanolamines?
Primary effects? |
Dimenhydrinate (Dramamine) and Diphenhydramine (Benadryl)
sedative;anti-cholinergic |
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What is an example of an ethylenediamine? Effects?
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Pyrilamine (Neo-Antergan)
GI effects |
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The two piperazines are:
Effects? |
Hydroxyzine (atarax)
Cyclizine (Merezine) Anxiolytic, motion sickness |
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Two alkylamines:
effects: |
Bromopheniramine (Dimentane)
Chloropheniramine (Chlor-Trimenton) OTC cold meds |
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A phenothiazine:
Effects: |
Promethazine (Phenergan)
CNS effects (anticholinergic, sedative, anti-emetic) |
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Lortadine (Claritin), Cetirizine (Zyrtec) and Fexofenadine (Allegra) all do what?
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Anti-allergy, second gen, longer half life
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The histamine-induced triple response is characterized by:
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Redness, wheal and flare
(local vasodilation, edema, neighboring vasodilation) |
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Located mostly in enterochromaffin cells and GI tract, and also in platelets and CNS
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5HT-Serotonin
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5HT is synthesized from which amino acid?
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Tryptophan
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What are the two steps in 5HT formation?
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1.Tryptophan hydroxylation
(trp-5-hydroxylase, rate limiting) 2.Decarboxylation-->5HT (aromatic L-amino acid decarboxylase) |
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This substance functions as a neurotransmitter, a precursor for melatonin, regulates GI motility and hemostasis and is degraded by MAO
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Serotonin (5HT)
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Which serotonin receptors are located in the cardiovascular system? What are the effects upon serotonin binding?
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5HT-2-->constricts SM in vessels in pulmonary and renal beds, but DILATES skeletal muscle and coronary vessels via NO release
5HT-3-->coronary vagal depolarization causes reflex hypotension and bradycardia |
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Which serotonin receptors are located in the GI tract? What is the effect of serotonin binding?
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5HT-2-->contracts intestinal smooth muscle (incr. IP3)
5HT-4-->on enteric nerves, causing Ach release and increased intestinal motility |
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Which serotonin receptors are located in the airways? What is the effect of serotonin binding?
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5HT-2-->contracts bronchial smooth muscle (incr. IP3), can cause hyperventilation due to chemoreceptor reflec or stim of bronchial sensory nerve endings
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Which serotonin receptors are located on the nerve endings? What is the effect of serotonin binding?
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5HT-1-->adrenergic terminals, INHIBITS nerve-stimulated NE release (decreases cAMP)
5HT-3-->vagal nerve terminals, CNS, can cause NAUSEA/VOMITING, pain, itching, respiratory stim and cardio reflexes |
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Why does chemotherapy induce nausea and vomiting? What can be done to treat this?
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During chemo, mucosal enterochromffin cells release Serotonin, which stimulates 5HT-3 receptors on vagus-->vomiting
Tx with a 5HT-3 antagonist such as Ondansetron or Granisetron. |
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Which serotonin agonist is used as a non-benzodiazapine anxiolytic? Which receptor does it agonize?
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Buspirone, 5HT-1 (CNS)
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Name 4 serotonin agonists that are used to treat migraine, and which receptor they are agonizing.
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-triptans
1. Sumatriptan 2. Naratriptan 3. Rizatriptan 4. Zolmitriptan Stimulate 5HT-1 (CNS, decr. cAMP and cause constriction of carotid arteriovenous anastamoses) |
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Cisapride activates the 5HT4 receptor to treat what?
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GERD
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A treatment for cold-induced urticaria, carcinoid syndrome and post-gastrectomy dumping syndrome that blocks 5HT-2 receptors:
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Cyproheptadine
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A drug that blocks 5HT2 receptors and is used in Europe for Raynaud's syndrome, some HTN, and intermittent claudication :
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Ketanserin
(Ritaserin sim, but without alpha-1 receptor antagonist properties) |
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A treatment for migraine headaches that antagonizes 5HT-2 receptors and often causes rebound headaches when withdrawn:
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Methysergide
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Clozapine is a treatment for Schizophrenia which blocks which receptor?
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5HT-6,7 (decr. cAMP, normally incr. by stim of this receptor)
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Plasma kallikrein catalyzes the transformation of a kiniogen (Kallidin) into:
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Bradykinin
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Kinins function as what:
Due to their fx, what can they cause: |
potent vasodilators
contract smooth muscle hypotension edema |
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Do kinins directly affect the heart?
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NO. Only indirectly, because kinins decrease TPR, and thereby cause REFLEX increase in CO and HR.
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The B1 kinin receptor functions in what:
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inflammation-induced receptor, causing smooth muscle contraction, collagen synthesis and cell multiplication
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The B2 kinin receptor is involved in what:
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Vasodilation, vascular permeability, non-vasc SM contraction
Produce multiple signal transduction events to prod effects, including Ca2+ mobilization, NO formation, adenylate cyclase formation |
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A Kallikrien inhibitor that is selective for B2 antagonist activity to inhibit pain and inflammation, especially in cardiothoracic surgery:
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Aprotinin
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