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66 Cards in this Set

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A muscarinic agonist that is non-specific and short-lived. Used in glaucoma tx to open the Canal of Schlemm.
A more specific muscarinic agonist that is rarely used.
A non-specific muscarinic agonist that through the addition of an amide is cholinesterase resistant. Treats glaucoma.
A tertiary amine M1 agonist used in the tx of glaucoma with profound diaphoretic (sweating) effects.
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.
You should not prescribe Bethanochol if your patient has the following conditions:

Hyperthyroidism, peptic ulcer, asthma, bradycardia, heart defects/disease, GI obstructions

Muscarinic Agonist that stimulates PNS
Indirect muscarinic agonists function by inhibiting:
Acetylcholine Esterase
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.
An indirect muscarinic agonist that is a reversible inhibitor of AchE (binds ionic site) and is used in diagnosis of myasthenia gravis
Edrophonium Chloride
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)
An indirect muscarinic agonist that is an organophosphate and irreversible inhibitor of AchE used to treat resistant glaucomas.
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.
What do cardiologists typically use to treat excessive vagal tone, reduce reflex bradycardia, but has side effects consistent with PNS inhibition?
A muscarinic antagonist that antagonizes bronchial muscarinic receptors for the treatment of COPD, emphysema, rhinitis and chronic bronchitis:
Ipratropium Br
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.
Propantheline Br
A muscarinic antagonist that was once used as an obstetric anesthetic that now is used to prevent motion sickness.
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.
A newer muscarinic antagonist that is a selective M3 blocker used to increase warning time of urinary urge in pts with urinary incontinence.
A nicotinic agonist used to aid in smoking cessation and targeting memory in Alzheimer's patients (Vernicidine):
When using nicotine gum as smoking cessation therapy, what food products should patients avoid and why?
Nicotine gum is reliant of alkaline saliva. So, pts should not consume acidic beverages like coffee and cola.
A nicotinic antagonist similar to trimethaphan and mecamylamine used as autonomic blockers in the tx of HTN and surgical bleeding.
This class of drugs are used as paralytic agents in intubations, setting broken bones, and delicate surgery:
Neuromuscular blockers
A depolarization blocker that functions by overstimulation depolarization that is short-lived (30sec) with fasiculation when given too rapidly.
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.
A NM blocker with a 10m half-life and mild histamine release. Metabolized by plasma esterase.
A NM blocker with a 50min half-life and some vagal ganglion blockade. Hepatically metabolized.
A NM blocker GABA-mimicking agonist which is is used as an antispastic in spinal cord lesions, multiple sclerosis, and trigeminal neuralgia
A NM blocker sedative, hypnotic and anxiolytic medication that enhances GABA binding for joint disease or muscle spasm.
Diazepam (don't give with EtOH as action amplified)
An NM blocker that reduces contraction by decreasing Ca2+ levels and is a treatment for Malignant Hyperthermia
Autocoid drug used to treat allergies, motion sickness and nausea and vomiting of pregnancy:
H1 Antihistamines
Which cause more sedation:
1st generation antihistimines
2nd generation antihistimines
1st gen
Drugs that target H1 receptors are called:
Fexofenadine and cetirizine target H1 and are used in what types of reactions?
Meclizine, Promethazine and Diphenhydramine target H1 and are used for what?
Anti-emetics (motion sickness, nausea, vertigo)
Promethazine and Diphenhydramine are best used for what?
Local anesthetic effects are more effective with which two antihistimines?
Promethazine and Diphenhydramine
All second generation antihistimines are indicated for what?
Which are the two ethanolamines?
Primary effects?
Dimenhydrinate (Dramamine) and Diphenhydramine (Benadryl)

What is an example of an ethylenediamine? Effects?
Pyrilamine (Neo-Antergan)

GI effects
The two piperazines are:

Hydroxyzine (atarax)
Cyclizine (Merezine)

Anxiolytic, motion sickness
Two alkylamines:

Bromopheniramine (Dimentane)
Chloropheniramine (Chlor-Trimenton)

OTC cold meds
A phenothiazine:

Promethazine (Phenergan)

CNS effects (anticholinergic, sedative, anti-emetic)
Lortadine (Claritin), Cetirizine (Zyrtec) and Fexofenadine (Allegra) all do what?
Anti-allergy, second gen, longer half life
The histamine-induced triple response is characterized by:
Redness, wheal and flare
(local vasodilation, edema, neighboring vasodilation)
Located mostly in enterochromaffin cells and GI tract, and also in platelets and CNS
5HT is synthesized from which amino acid?
What are the two steps in 5HT formation?
1.Tryptophan hydroxylation
(trp-5-hydroxylase, rate limiting)
(aromatic L-amino acid decarboxylase)
This substance functions as a neurotransmitter, a precursor for melatonin, regulates GI motility and hemostasis and is degraded by MAO
Serotonin (5HT)
Which serotonin receptors are located in the cardiovascular system? What are the effects upon serotonin binding?
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
Which serotonin receptors are located in the GI tract? What is the effect of serotonin binding?
5HT-2-->contracts intestinal smooth muscle (incr. IP3)
5HT-4-->on enteric nerves, causing Ach release and increased intestinal motility
Which serotonin receptors are located in the airways? What is the effect of serotonin binding?
5HT-2-->contracts bronchial smooth muscle (incr. IP3), can cause hyperventilation due to chemoreceptor reflec or stim of bronchial sensory nerve endings
Which serotonin receptors are located on the nerve endings? What is the effect of serotonin binding?
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
Why does chemotherapy induce nausea and vomiting? What can be done to treat this?
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.
Which serotonin agonist is used as a non-benzodiazapine anxiolytic? Which receptor does it agonize?
Buspirone, 5HT-1 (CNS)
Name 4 serotonin agonists that are used to treat migraine, and which receptor they are agonizing.
1. Sumatriptan
2. Naratriptan
3. Rizatriptan
4. Zolmitriptan
Stimulate 5HT-1 (CNS, decr. cAMP and cause constriction of carotid arteriovenous anastamoses)
Cisapride activates the 5HT4 receptor to treat what?
A treatment for cold-induced urticaria, carcinoid syndrome and post-gastrectomy dumping syndrome that blocks 5HT-2 receptors:
A drug that blocks 5HT2 receptors and is used in Europe for Raynaud's syndrome, some HTN, and intermittent claudication :

(Ritaserin sim, but without alpha-1 receptor antagonist properties)
A treatment for migraine headaches that antagonizes 5HT-2 receptors and often causes rebound headaches when withdrawn:
Clozapine is a treatment for Schizophrenia which blocks which receptor?
5HT-6,7 (decr. cAMP, normally incr. by stim of this receptor)
Plasma kallikrein catalyzes the transformation of a kiniogen (Kallidin) into:
Kinins function as what:

Due to their fx, what can they cause:
potent vasodilators
contract smooth muscle

Do kinins directly affect the heart?
NO. Only indirectly, because kinins decrease TPR, and thereby cause REFLEX increase in CO and HR.
The B1 kinin receptor functions in what:
inflammation-induced receptor, causing smooth muscle contraction, collagen synthesis and cell multiplication
The B2 kinin receptor is involved in what:
Vasodilation, vascular permeability, non-vasc SM contraction

Produce multiple signal transduction events to prod effects, including Ca2+ mobilization, NO formation, adenylate cyclase formation
A Kallikrien inhibitor that is selective for B2 antagonist activity to inhibit pain and inflammation, especially in cardiothoracic surgery: