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219 Cards in this Set
- Front
- Back
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Ganciclovir (DHPG dihydroxy-2-propoxymethyl guanine)
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p300
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Mechanism of action of Ganciclovir.
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Phosphorlation by viral kinase; perferentially inhibits CMV DNA polymerase.
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Clinical use of Ganciclovir.
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CMV, especially in immunocompromised patients.
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Symptoms of Ganciclovir toxicity.
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Leukopenia, neutropenia, thrombocytopenia, renal toxicity. More toxic to host enzymes than acyclovir.
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Foscarnet
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p300
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Mechanism of action of Foscarnet.
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Viral DNA polymerase inhibitor that binds to the pyrophophate binding site of the enzyme. Does not require activation by viral kinase. "FOScarnet = pyroFOSphate analog."
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Clinical use of Foscarnet.
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CMV retinitis in immunocompromised patients when ganciclovir fails.
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Symptoms of Foscarnet toxicity.
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Nephrotoxicity.
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HIV therapy
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p300
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Saquinavir, ritonavir, indinavir, nelfinavir, amprenavir are example of this type of anti-HIV drug.
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Protease inhibitor.
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Mechanism of action of protease inhibitors.
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Inhibit assembly of new virus by blocking protease enzyme.
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Symptoms of protease inhibitor toxicity.
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GI intolerance (nausea, diarrhea), hyperglycemia, lipid abnormalities, thrombocytopenia (indinavir).
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Reverse transcriptase inhibitors:
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Zidovudine (AZT), didanosine (ddI), zalcitabine (ddC), stavudine (d4T), lamivudine (3TC), and abacavir are examples of --------- reverse transcriptase inhibitors.
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Nucleoside.
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Nevirapine, delavirdine, and efavirenz are examples of --------- reverse transcriptase inhibitors.
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Non-nucleoside.
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Mechanism of action of reverse transcriptase inhibitors.
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Preferentially inhibit reverse transcriptase of HIV; prevent incorporation of viral genome into host DNA.
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Symptoms of reverse transcriptase inhibitor toxicity.
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Bone marrow supression (neutropenia, anemia), periphral neuropathy, lactic acidosis (nucleosides), rash (non-nucleosides), megaloblastic anemia (AZT).
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Highly active antiretroviral therapy (HAART) generally entails combination therapy with ---------- and -----------.
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Protease inhibitors, reverse transcriptase inhibitors.
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When should HIV therapy be initiated?
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When patients have low CD4 counts (<500 cells/mm3) or high viral load.
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-------- is used during pregnancy to reduce risk of fetal transmission.
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AZT.
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Interferons
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p300
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Mechanism of action of Interferons.
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Glycoproteins from human leukocytes that block various stages of viral RNA and DNA synthesis.
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Clinical use of Interferons.
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Chronic hepatitis B and C, Kaposi's sarcoma.
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Symptoms of Interferon toxicity.
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Neutropenia.
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Antiparasitic drugs
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p301
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Clinical uses of Ivermectin.
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Onchocerciasis "rIVER blindness treated with IVERmectin".
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Clinical uses of Mebendazole / thiabendazole.
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Nematode/roundworm (e.g., pinworm, whipworm) infections.
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Clinical uses of Pyrantel pamoate.
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Giant roundworm (Ascaris), hookworm (Necator/Ancylostoma), pinworm (Enterobius).
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Clinical uses of Praziquantel.
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Trematode/fluke (e.g., schistosomes, Paragonimus, Clonorchis) and cysticercosis.
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Clinical uss of Niclosamide
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Cestode/tapeworm (e.g., Diphyllobothrium latum, Taenia species) infections except cysticercosis.
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Clinical uses of Pentavalent antimony.
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Leishmaniasis.
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Clinical uses of Chloroquine, quinine, mefloquine, atovaquone, proguanil.
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Malaria.
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Clinical uses of Primaquine.
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Latent hypnozoite (liver) forms of malaria (Plasmodium vivax, P.ovale).
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Clinical uses of Metronidazole.
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Giardiasis, amebic dysentery (Entamoeba histolytica), bacterial vaginitis (Gardnerella vaginalis), Trichomonas.
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Clinical uses of Pentamidine.
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Pneumocystis carinii pneumonia prophylaxis.
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Clinical uses of Nifurtimox.
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Chagas' disease, American trypanosomiasis (Trypanosoma cruzi).
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Clinical uses of Suramin.
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African trypanosomiasis (sleeping sickness).
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Pharmacology - CNS / Neurologic drugs
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p301
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Parasympathetic preganglionic neurons release the neurotransmitter -------- which act on -------- receptors.
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Ach, nicotinic.
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Parasympathetic postganglionic neurons release the neurotransmitter -------- which act on ------- receptors.
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Ach, muscarinic.
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Sympathetic preganglionic neurons to sweat glands release the neurotransmitter ------- which act on ------- receptors.
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Ach, nicotinic.
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Sympathetic postganglionic neurons to sweat glands release the neurotransmitter ------- which act on ------- receptors.
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Ach, muscarinic.
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Sympathetic preganglionic neurons to glands, cardiac and smooth muscles release the neurotransmitter ------- which act on ------- receptors.
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Ach, nicotinic.
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Sympathetic postganglionic neurons to glands, cardiac and smooth muscles release the neurotransmitter ------- which act on ------- receptors.
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NE, alpha and beta
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Sympathetic preganglionic neurons to renal vascular smooth muscle release the neurotransmitter ------- which act on ------- receptors.
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Ach, nicotinic.
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Sympathetic postganglionic neurons to renal vascular smooth muscle release the neurotransmitter ------- which act on ------- receptors.
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Dopamine, D1
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Sympathetic preganglionic neurons to the adrenal medulla release the neurotransmitter ------- which act on ------- receptors.
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Ach, nicotinic.
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Sympathetic preganglionic neurons to the adrenal medulla synapse directly on ------- cells of the adrenal medulla.
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Chromaffin.
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Somatic neurons synapse directly on -------- muscle and release the neurotransmitter ------- which act on ------- receptors.
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skeletal muscle, Ach, nicotinic.
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Autonomic drugs
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p302
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Cholinergic:
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Ach is synthesized from acetyl-CoA and choline by the enzyme ---------.
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Choline acetyltransferase.
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The transport of choline into the nerve terminal can be inhibited by --------.
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Hemicholinium.
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The release of transmitter from vesicles in the nerve ending require the entry of ------ into the neuron.
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Calcium.
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#NAME?
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Botulinum toxin.
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The action of Ach in the synapse is terminated by its metabolism to acetate and choline by the enzyme ---------.
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Acetylcholinesterase.
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Noradrenergic:
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In the noradrenergic nerve terminal, tyrosine is hydroxylated to -------, which is decarboxylated to --------, which is finally hydroxylated to NE.
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DOPA, dopamine.
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Dopamine is transported into vesicles for hydroxylation to NE. This transport can be blocked by the drug --------.
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Reserpine.
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The action of NE and DA is terminated by --------- and ----------.
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Reuptake, diffusion (different than for Ach).
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--------- inhibits the release of the stored NE.
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Guanethidine.
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The --------- drugs promote catecholamine release.
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Amphetamine.
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The drugs --------- and ---------- inhibit the reuptake of NE.
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Cocaine, TCA.
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The release of NE from a sympathetic nerve ending is modulated by ---------, --------- and ---------.
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NE, Ach, angiotensin II.
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NE inhibits its own release at the noradrenergic nerve terminal through --------- receptors.
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Alpha 2.
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Angiotensin II --------- (inhibits / stimulates) the release of NE from the noradrenergic nerve terminal.
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Stimulates.
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Ach inhibits the release of NE from the noradrenergic nerve terminal by binding to --------- receptors.
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M1.
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Cholinomimetics
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p303
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Direct agonists:
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Clinical application and action of Bethanechol.
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Postoperative and neurogenic ileus and urinary retention. / Activates bowel and bladder smooth muscle.
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Clinical application and action of Carbachol and Pilocarpine.
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Glaucoma. / Activates ciliary muscle of eye (open angle), pupillary sphincter (narrow angle).
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Indirect agonists (anticholinesterases):
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Clinical application / action of Neostigmine.
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Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative). / Increase endogenous Ach.
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Clinical application / action of Pyridostigmine.
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Myasthenia gravis. / Increase Ach; increase strength.
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Clinical application / action of Edrophonium.
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Diagnosis of myasthenia gravis (extremely short acting). / Increase endogenous Ach.
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Clinical application / action of Physostigmine.
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Glaucoma (crosses blood-brain barrier) and atropine overdose. / Increase endogenous Ach.
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Clinical application / action of Echothiophate.
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Glaucoma. / Increase endogenous Ach.
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Symptoms of cholinesterase inhibitor poisoning.
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Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation (also abdominal cramping). "DUMBBELSS".
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Cholinesterase inhibitor poisoning may be caused by ---------.
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Parathion and other organophosphates.
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The cholinesterase regenerator ------- can be used as an antidote for cholinesterase inhibitor poisoning.
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Pralidoxime.
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Mechanism of action of Pralidoxime.
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Regenerates active cholinesterase, chemical antagonist, used to treat organophosphate exposure.
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Cholinoreceptor blockers:
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p303
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Clinical uses of the muscarinic antagonist Atropine.
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Dilate pupils, decrease acid secretion in peptic ulcer disease, decrease urgency in mild cystitis, decrease GI motility, reduce airway secretions, and treat organophosphate poisoning. "Blocks SLUD: Salivation, Lacrimation, Urination, Defecation."
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Side effects of Atropine.
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Increase body temp, rapid pulse, dry mouth, dry/flushed skin, disorientation, mydriasis with cycloplegia, and constipation. "Atropine parasympathetic block side effects: Blind as bat, Red as a beet, Mad as a hatter, Hot as a hare, Dry as a bone."
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Hexamethonium (ganglionic blocker) blocks -------- receptors.
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Nicotinic.
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AUTHOR
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Tzivia Moreen
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antimuscarinic drugs
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p. 304
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tropi are anti-muscarinic
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while vacationing in the tropics you lie on a beach and your muscles waste away!
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benztropine is used to treat
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Parkinson's disease
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scopolamine is used to treat
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motion sickness
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scopolamine is an antimuscarinic that does not convert to the mnemonic!
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name 2 antimuscarinic drugs that act on the CNS
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benztropine, scopolamine
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name a muscarinic used to treat motion sickness
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scopolamine
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name a muscarinic used to treat Parkinson's disease
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benztropine
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mechanism of action of benztropine
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antimuscarinic
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mechanism of action of scopolamine
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antimuscarinic
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name three antimuscarinics that act on eye
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atropine, homatropine, tropicamide
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the action of atropine is ______
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produce mydriasis, cycloplegia
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mechanism of atropine is
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antimuscarinic
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the action of homatropine is ______
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produce mydriasis, cycloplegia
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mechanism of homatropine is
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antimuscarinic
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the action of tropicamide is
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produce mydriasis, cycloplegia
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mechanism of tropicamide is
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antimuscarinic
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ipatropium is used to treat
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asthma, COPD
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mechanism of ipatropium is
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antimuscarinic
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name an antimuscarinic used to treat asthma and COPD
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ipatropium
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neuromuscular blocking drugs
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p. 304
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neuromuscular blocking drugs are used for
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muscle paralysis in surgery or mechanical ventilation
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name a depolarising neurmuscular blocking drug
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succinylcholine
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name 6 nondepolarizing neuromuscular blocking drugs
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tubocurarine
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*mnemonic -- the "cur" drugs are nondepolarizing neuromuscular blocking agents
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atracurium
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is succinylcholine depolarizing or nondepolarizing?
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depolarizing
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is tubocurarine depolarizing or nondepolarizing?
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nondepolarizing
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is atracurium depolarizing or nondepolarizing?
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nondepolarizing
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is mivacurium depolarizing or nondepolarizing?
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nondepolarizing
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is pancuronium depolarizing or nondepolarizing?
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nondepolarizing
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is vacuronium depolarizing or nondepolarizing?
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nondepolarizing
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is rapacuronium depolarizing or nondepolarizing?
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nondepolarizing
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what is tubocurarine used for
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nondepolarizing neuromuscular blockade
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what agents are used to reverse neuromuscular blockade by succinylcholine?
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cholinesterase inhibitors in phase II (ex -- neostigmine)
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what phase of succinylcholine neuomuscular bloackade is reversible?
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phase II (repolarized but blocked)
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what agents are used to reverse pahse I neuromuscular blockade by succinylcholine?
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phase I Succinylcholine neuromuscular blockade cannot be reversed
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what phase of succinylcholine neuomuscular bloackade is irreversible?
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phase I Succinylcholine neuromuscular blockade cannot be reversed
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what is atracurium used for
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nondepolarizing neuromuscular blockade
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what is the effect of cholinesterase inhibitors on succinylcholine neuromuscular blockade?
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phase I: cholinesterase inhibitors potentiates the blockade phase II: cholinesterase inhibitors reverse the blockade
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what cholinesterase inhibitor is used to reverse phase II of succinylcholine neuromuscular blockade?
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neostigmine
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what is mivacurium used for
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nondepolarizing neuromuscular blockade
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Dantrolene
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p. 304
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what is dantrolene used for
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treat malignant hyperthermia
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what causes malignant hyperthermia
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use inhalation anesthetics and succinylcholine together
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what inhalation anesthetic DOES NOT cause malignanat hyperthermia?
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N2O
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what is dantrolene used for
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neuroleptic malignant syndrome
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what is neuroleptic malignant syndrome
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a toxicity of antipsychotic drugs
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what drug is used to treat malignant hyperthermia
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dantrolene
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what is the mechanism of dantrolene
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prevents release of Ca++ from saarcoplasmic reticulum of skeletal muscle
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Sympathomimetics
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p. 305
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epinephrine, NE, isoproterenol, dopamine, and dobutamine are all________________
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catecholamines
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catecholamines are_____________________
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sympathomimetics
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name 5 catecholamines
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EPI, NE, Isoproterenol, dopamine, dobutamine
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what receptors does epinephrine act on?
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alpha-1, alpha-2, beta-1, beta-2 adrenergics
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what receptors does NE work on?
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alpha-1, alpha-2, beta-1 adrenergics
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what receptors does isoproterenol work on?
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beta-1 = beta-2 adrenergics
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what receptors does dopamine work on?
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D1 = D2, D1 and D2 more than beta, beta more than alpha
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what receptors does dobutamine work on?
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beta-1 > beta-2
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which catecholamines are agonists to alpha-adrenergic receptors
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EPI, NE > dopamine
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which catecholamines are agonists to beta-1 adrenergic receptors
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EPI, NE, Isoproterenol, dopamine, dobutamine
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which catecholamines are agonists to beta-2 adrenergic receptors
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EPI, isoproterenol, dopamine and dobutamine (less)
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what is epinephrine used to treat?
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anaphylaxis, open-angle glaucoma, asthma, hypotension
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what is norepinephrine used to treat?
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hypotension (but decreases renal perfusion)
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what is isoproterenol used to treat?
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AV block
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what is dopamine used to treat
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shock with renal failure, heart failure
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what is dobutamine used to treat
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shock, heart failure
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what catecholamine is used to treat anaphylaxis
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epinephrine ("EPI-pen")
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what catecholamines are used to treat hypotension
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EPI, NE
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what catecholamine is used to treat asthma
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epinephrine
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what catecholamine is used to treat AV block
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isoproterenol
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what catecholamines are used to treat shock
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doapmine, dobutamine
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what is the action of amphetamine
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indirect general adrenergic agonist, releases stored catecholamines
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what is the action of ephedrine
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indirect general adrenergic agonist, releases stored catecholamines
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what is amphetamine used to treat
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narcolepsy, obesity, attention deficit disorder
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what is ephedrine used to treat
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nasal decongestion, urinary incontinence, hypotension
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name three sympathomimetic drugs used to treat hypotension
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epinephrine, norepinephrin, ephedrine
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what is the action of phenylephrine
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adrenergic agonist, alpha-1 > alpha-2
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what is the action of albuterol
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adrenergic agonist, beta-2 >beta-1
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what is the action of terbutaline
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adrenergic agonist, beta-2 >beta-2
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what is phenylephrine used for?
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pupil dilator, vasoconstriction, nasal decongestion
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what sympathomimetics are used to treat nasal congestion
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ephedrine, phenylephrine
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what is the mechanism of cocaine
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indirect general adrenergic agonist, catecholamine uptake inhibitor
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what is the action of cocaine
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vasoconstriction, local anesthesia
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what is the mechanism of clonidine
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centrally acting alpha-adrenergic agonist, decreases central adrenergic outflow
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what drug has the same mechanism as amphetamine
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ephedrine
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what is the mechanism of alpha-methyldopa
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centrally acting alpha-adrenergic agonist, decreases central adrenergic outflow
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what drug has the same mechanism as clonidine
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alpha-methyldopa
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what are clonidine and alpha-methyldopa used to treat
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hypertension, especially in renal disease because they do not decreased blood flow to the kidney
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what sympathomimetic is used to treat urinary incontinence
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ephedrine
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what sympathomimetic is used to treat attention deficit disorder
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amphetamine
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what sympathomimetic is used to treat narcolepsy
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amphetamine
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alpha-blockers
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p. 306
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name a nonselective irreversible alpha blocker
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phenoxybenzamine
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name a nonselective reversible alpha blocker
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phentolamine
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what is the mechanism of phenoxybenzamine
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nonselective irreversible alpha blocker
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what is the mechanism of phentolamine
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nonselective reversible alpha blocker
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what are phenoxybenzamine and phentolamine used for
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pheochromocytoma
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what are the side effects of nonselective alpha blockers
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orthostatic hypotension, reflex tachycardia
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name 3 alpha-1 selective adrenergic blockers
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prazosin, terazosin, doxazosin
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what is the mechanism of prazosin
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alpha-1 selective adrenergic blocker
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what is the mechanism of terazosin
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alpha-1 selective adrenergic blocker
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what is the mechanism of doxazosin
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alpha-1 selective adrenergic blocker
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what are alpha-1 selective adrenergic alpha blockers used for
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hypertension, urinary retention in BPH
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what are the side effects of alpha-1 blockers
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orthostatic hypotension, dizziness, headache
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what is prazosin used for?
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hypertension, urinary retention in BPH
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what drugs have the same action as prazosin
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terazosin, doxazosin
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what are the side effects of terazosin?
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orthostatic hypotension, dizziness, headache
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what selective alpha blockers cause orthostatic hypotension
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phenoxybenzamine, phentolamine, terazosin, prazosin, doxazosin
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name an alpha-2 selective adrenergic blocker
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yohimbine
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what is yohimbine used for
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impotence (effectiveness controversial)
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what alpha blockers are used to treat pheochromocytoma
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phenoxybenzamine, phentolamine
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beta-blockers ("lol"s)
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p. 307
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name some beta-blockers
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propranolol, metoprolol, atenolol, nadolol, timolol, pindolol, esmolol, labetalol
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what is the mechanism of propanolol
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selective beta-adrenergic blocker
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what is the mechanism of metoprolol
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selective beta-adrenergic blocker
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what is the mechanism of esmolol
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selective beta-adrenergic blocker
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what is the mechanism of pindolol
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selective beta-adrenergic blocker
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what are beta-blockers used to treat
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hypertension, angina, MI, SVT, CHF, glaucoma
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how do beta blockers treat hypertension
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decrease cardiac output, decrease renin secretion
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how do beta blockers treat angina
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decrease heart rate, decrease cardiac contractility, decreased O2 consumption
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why are beta blockers used to treat MI
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decrease MI mortality
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which beta blockers are used to treat SVT
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propanolol, esmolol
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how do propanolol and esmolol treat SVT
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decrease AV conduction velocity
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how do beta blockers treat CHF
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slow progression of chronic failure
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which beta blocker is used to treat glaucoma
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timolol
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what is timolol used to treat glaucoma
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decrease secretion of aqueous humor
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what are the toxic effects of beta blockers
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impotence, exacerbation of asthma, caution in diabetes
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what are the cardiovascular toxic effects of beta blockers
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bradychardia, AV block, CHF
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what are the CNS adverse effects of beta blockers
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sedation, sleep alterations
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which beta blockers are beta-1 selective
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acebutolol, betaxolol, esmolol, atenolol, metaprolol (A BEAM of beta-1 blockers)
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which beta-1 blocker is short-acting
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esmolol
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which beta blockers are non-selective
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propanolol, timolol, pindolol, nadolol, labetalol
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which beta blocker also blocks alpha receptors
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labetalol (all others are spelled "olol")
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