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84 Cards in this Set
- Front
- Back
Methacholine
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• Choline ester Specific ONLY for muscarinic receptors
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Carbachol
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Direct Acting Cholinergic Agonist
• Resistant to AChE (longer duration) |
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Bethanechol
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• Resistant to AChE (longer duration) AND
• Specific ONLY for muscarinic receptors |
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Pilocarpine (Cevilemine)
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• Stimulation of M3 receptors causes contraction of iris sphincter muscle (miosis)
• Contraction of ciliary muscle causes lens thickening • Combination allows lowering of ocular pressure and outflow of aqueous humor through Canal of Schlemm |
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Isoflurophate
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- POISON - IRREVERSIBLE Indirect Acting Agonist (AChE inhibitor)
- Can lead to poisoning: excess ACh activity in CNS, PNS - Reversal by antidote: PRALIDOXIME |
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Echothiophate
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- Poison - IRREVERSIBLE Indirect Acting Agonist (AChE inhibitor)
• Used for biological warfare • Can lead to poisoning: excess ACh activity in CNS, PNS - Reversal by antidote: PRALIDOXIME** (+ atropine to reverse CNS effects) |
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PRALIDOXIME
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antidote for irreversible AChE inhibitors
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Edrophonium
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REVERSIBLE AChE inhibitor
Used as a diagnostic test for myasthenia gravis |
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Pyridostigmine
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REVERSIBLE AChE inhibitor
Used to maintain therapeutic effects during treatment of myasthenia gravis |
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Neostigmine and Ambenonium
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REVERSIBLE AChE inhibitor
Treatment of: • Postoperative ileus • Congenital megacolon • Urinary retention due to surgery, spinal injury, disease • Reflux esophagitis |
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Physostigmine
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REVERSIBLE AChE inhibitor
Treatment of: • Glaucoma • Atropine poisoning |
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Carbaryl
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REVERSIBLE AChE inhibitor
• Insecticide |
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Atropine
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Muscarinic (M) Receptor Antagonist
• Effective in blocking exogenously administered cholinergic agonists • TOXIC in high doses "atropine fever" • Eye: dilation = mydriasis, paralyze ciliary muscle = Cycloplegia |
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"Atropine fever”
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loss of sweating (cholinergic sympathetics to sweat glands) leading to dangerously elevated temperature
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Ipratropium
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Muscarinic (M) Receptor Antagonist
Like atropine |
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Scopolamine
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Muscarinic (M) Receptor Antagonist
• More sedative effects than atropine • Patch for motion sickness |
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Tubocararine
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NON-DEPOLARIZING BLOCKER
Neuromuscular Junction (NM) Receptor Antagonist • Produce a competitive blockade via binding at nicotinic receptor site to compete with the natural transmitter ACh • Adjuncts in surgery that require general anesthesia • Enable muscle relaxation without the need to produce dangerously deep anesthesia |
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Metocurine
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NON-DEPOLARIZING BLOCKER
Neuromuscular Junction (NM) Receptor Antagonist • Produce a competitive blockade via binding at nicotinic receptor site to compete with the natural transmitter ACh • Adjuncts in surgery that require general anesthesia • Enable muscle relaxation without the need to produce dangerously deep anesthesia |
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Pancuronium
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NON-DEPOLARIZING BLOCKER
Neuromuscular Junction (NM) Receptor Antagonist • Produce a competitive blockade via binding at nicotinic receptor site to compete with the natural transmitter ACh • Adjuncts in surgery that require general anesthesia • Enable muscle relaxation without the need to produce dangerously deep anesthesia |
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Gallamine
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NON-DEPOLARIZING BLOCKER
Neuromuscular Junction (NM) Receptor Antagonist • Produce a competitive blockade via binding at nicotinic receptor site to compete with the natural transmitter ACh • Adjuncts in surgery that require general anesthesia • Enable muscle relaxation without the need to produce dangerously deep anesthesia |
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Vecuronium
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NON-DEPOLARIZING BLOCKER
Neuromuscular Junction (NM) Receptor Antagonist • Produce a competitive blockade via binding at nicotinic receptor site to compete with the natural transmitter ACh • Adjuncts in surgery that require general anesthesia • Enable muscle relaxation without the need to produce dangerously deep anesthesia |
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Succinylcholine
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DEPOLARIZING BLOCKER Neuromuscular Junction (NM) Receptor Antagonist
non-competitive • Adjuncts in surgery that require general anesthesia • Enable muscle relaxation • Genetic variations of Pseudocholinesterase may result in longer duration of action of succinylcholine |
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Phase I block
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produced by persistent ACh-like action of succinylcholine at NM receptor site – open channel, leading to persistent end-plate depolarization and initial desynchronized muscle contractions
• Because of persistent depolarization of end-plate, subsequent contracts CANNOT occur |
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Phase II block
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- end-plate repolarizes despite presence of succinylcholine. But, end-plate has become “DESENSITIZED” and channel remains in prolonged closed state
• Terminated by hydrolysis by AChE & Pseudocholinesterase |
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Mecamylamine
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DEPOLARIZING BLOCKER
Nicotinic Ganglionic (Nn) Blocking Agent • Block actions of ACh at preganglionic nicotinic receptor of autonomic ganglia within the SYMP and PARA nervous systems limited only to emergency room management of hypertensive crisis and used for controlled hypotension during surgery |
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Trimethaphan
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DEPOLARIZING BLOCKER
Nicotinic Ganglionic (Nn) Blocking Agent • Block actions of ACh at preganglionic nicotinic receptor of autonomic ganglia within the SYMP and PARA nervous systems limited only to emergency room management of hypertensive crisis and used for controlled hypotension during surgery |
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Hexamethonium
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DEPOLARIZING BLOCKER
Nicotinic Ganglionic (Nn) Blocking Agent • Block actions of ACh at preganglionic nicotinic receptor of autonomic ganglia within the SYMP and PARA nervous systems limited only to emergency room management of hypertensive crisis and used for controlled hypotension during surgery |
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Epinephrine
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MIXED (a1 = a2; B1 = B2)
• CV: positive ionotropic action (B1) – increase force of contraction (CO) • CV: positive chronotropic action (B1) – increase rate of contraction (HR) • B1 - CO↑, HR↑, Systolic BP ↑ • B2 – increase vasodilation = TPR↓: Diastolic BP ↓* |
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Norepinephrine
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MIXED (a1 = a2; B1 >>> B2)
• B1 - CO↑, HR↓ (reflex bradycardia)** • B1 - Systolic BP ↑* • B2 no effect = no vasodilation = Diastolic BP ↑** |
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Isoproterenol
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BETA AGONIST
(B1 = B2 >>>> a) • Increase HR, increase SBP • Decrease TPR, decreased DBP • Similar effects as epinephrine |
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Dobutamine
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BETA 1 AGONIST
(B1 > B2 >>>>> a) • Increases HR and CO, SV • Short-term treatment of cardiac decompensation (after surgery, MI) |
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Terbutaline
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BETA 2 AGONIST
(B2 >> B1 >>>>>a) |
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Metaproterenol
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BETA 2 AGONIST
(B2 >> B1 >>>>>a) |
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Albuterol
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BETA 2 AGONIST
(B2 >> B1 >>>>>a) - Tolerance can develop by receptor down-regulation • Relieve bronchodilation • Treatment of asthma |
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Ritodrine
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BETA 2 AGONIST
(B2 >> B1 >>>>>a) • Uterine relaxant – prevention of premature labor & prolongs pregnancy |
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Salmeterol and Formoterol
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BETA 2 AGONIST
(B2 >> B1 >>>>>a) • LONGEST LASTING: 12 hour duration, but slower acting o Advair = salmeterol + fluticasone o Symbicort = formoterol + budesonide |
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Bitolterol
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PRODRUG
B2 AGONIST • Esterases in lung metabolize drug to active form: Colterol |
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Phenyleprine and Methoxamine
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ALPHA 1 AGONIST
(a1 > a2 >>>> B) • Nasal decongestant (less fluid through nasal passages due to vasoconstriction) • Opthalmic use: mydriatic – dilation of pupils • Can terminate episodes of supraventricular tachycardia • May cause hypertension |
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Pseudoephedrine (Sudafed)
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ALPHA 1 AGONIST
(a1 > a2 >>>> B) • Used in preparation of meth • Decongestant |
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Clonidine
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ALPHA 2 AGONIST
• Alpha 2 activation leads to presynaptic inhibition of NE release – inhibition of Sympathetic NS • Lowers blood pressure • Patch delivers constant rate for 1 week |
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Amphetamine
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MIXED EFFECTS; INDIRECT-ACTING DRUG
• Strong CNS stimulant • Reuptake into terminals and displace NE from vesicles leads to release of NE (indirect) |
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Prazosin
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ALPHA 1 ANTAGONIST
• Inhibitory feedback mechanism for NE • Less effect on baroreceptor reflex • Antihypertensive, without tachycardia or orthostatic hypotension |
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Terazosin
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ALPHA 1 ANTAGONIST
• Longer action than Prazosin • Antihypertensives • Relax muscle in prostate |
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Tamsulosin
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ALPHA 1 ANTAGONIST
- useful in BPH with little effect on BP |
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Propranolol
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NON-SELECTIVE BETA BLOCKER (no ISA)
• Effects (B1): o Blunt expected rise in HR (negative chronotropy) o Decrease force of contraction (negative inotropy) o Decreased conduction velocity in AV node o Decreased CO o Decreased cardiac work o Decreased BP (beta 2 activity) o Decreased O2 consumption o BENEFICIAL EFFECTS FOR ANGINA o inhibition of renin release o decreased intraocular pressure • Effects (B2): o Problems in asthmatics: bronchoconstriction o Problems in diabetics o Beneficial: antagonism of catecholamine-induced tremor |
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Nadalol
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NON-SELECTIVE BETA BLOCKER
• Long-acting (duration up to 24 hours) |
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Timolol
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NON-SELECTIVE BETA BLOCKER
• Useful in ophthalmic prep – open-angle glaucoma |
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Pindolol
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NON-SELECTIVE BETA BLOCKER (has ISA)
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Acebutolol
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SELECTIVE B1 BLOCKER (has ISA)
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Atenolol
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SELECTIVE B1 BLOCKER
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Metoprolol
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SELECTIVE B1 BLOCKER
• 1st pass metabolism by CYP2D6 – susceptible to pharmacogenetic modification |
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Nebivolol
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MOST SELECTIVE B1 BLOCKER
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Labetolol
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NON-SELECTIVE BETA BLOCKER + ALPHA 1 BLOCKER
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Carvedilol
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NON-SELECTIVE BETA BLOCKER + ALPHA 1 BLOCKER + Ca CHANNEL BLOCK
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Esmolol
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SELECTIVE B1 BLOCKER
• SHORTEST ACTING - Metabolized by esterases in blood, t½ is 10 mins |
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List four antivirals used to treat influenza
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1. Amantadine, 2. Rimantadine - mechanism: block uncoating of influenza A viruspreventing
penetration of virus into host 3. Relenza 4. Tamiflu - neuraminidase inhibitors |
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List two neuraminidase inhibitors
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Relenza
Tamiflu Inhibit influenza virus neuraminidase, an enzyme known to cleave the budding viral progeny from its cellular envelope attachment point |
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List the interferon used to treat hepatitis B
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Interferon alpha-2b
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Acyclovir (Zovirax)
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Mechanism: Inhibits DNA synthesis and
viral replication by being incorporated into viral DNA • Dental use: tx of recurrent mucosal and cutaneous herpes simplex infections in immunocompromised patients |
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Valacyclovir (Valtrex)
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• Mechanism: converted to acyclovir by hepatic enzymes then goes through mechanism
above • Dental use: tx of herpes labialis (cold sores) |
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Famciclovir (Famvir)
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Mechanism: converted to penciclovir to inhibit viral DNA synthesis
• Dental use: management of acute herpes zoster (shingles); tx of herpes labialis |
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Penciclovir (Denavir)
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Mechanism: inhibits viral DNA synthesis and replication
• Dental use: tx of herpes labialis; apply locally as cream to lesion |
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List the four subclasses of HIV drugs
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1. Nucleoside Reverse Transcriptase Inhibitors - (Retrovir)
2. Protease Inhibitors - Indinavir 3. Nonnucleoside Reverse Transcriptase Inhibitors - (Rescriptor) 4. Fusion Protein Inhibitors - (Fuzeon) |
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How do Nucleoside Reverse Transcriptase Inhibitors work against the HIV virus?
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Work by inhibiting the viral enzyme reverse transcriptase. Without reverse transcriptase, the viral RNA cannot be made into a DNA segment and DNA integration (chain elongation) does not take place.
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How do Protease Inhibitors work against the HIV virus?
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Inhibit protease, the enzyme responsible for cleaving viral precursor peptides into infective virions.
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How do the Nonnucleoside reverse transcriptase inhibitors work against the HIV virus?
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Inhibits the catalytic reaction of reverse transcriptase that is independent of nucleotide binding.
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How do Fusion Protein Inhibitors work against the HIV virus?
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Inhibits the fusion of HIV-1 virus with CD4 cells by blocking the conformational change in viral envelope fusion protein required for membrane fusion and entry into the CD4 cells.
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Using Zidovudine (Retrovir) as the example of a Nucleoside Reverse Transcriptase Inhibitors describe the use and unlabeled use from DIHD.
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Use: Treatment of HIV infection in combination with at least two other antiretroviral agents; prevention of maternal/fetal HIV transmission as monotherapy
Unlabeled Use: Postexposure prophylaxis for HIV exposure as part of a multidrug regimen. |
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Using Indinavir (Crixivan) as the example of a Protease Inhibitor describe the use from DIHD
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Treatment of HIV infection; should always be used as part of a multidrug regimen (at least three antiretroviral agents)
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7. Using Delavirdine (Rescriptor) as the example of a Nonnucleoside Reverse Transcriptase Inhibitor describe the use from DIHD.
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Treatment of HIV-1 infection in combination with at least two additional antiretroviral agents
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Using Enfuvirtide (Fuzeon) as the example of a Fusion Protein Inhibitor.describe the use from DIHD.
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Treatment of HIV-1 infection in combination with other antiretroviral agents in treatment-experienced patients with evidence of HIV-1 replication despite ongoing antiretroviral therapy
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Cancer drugs
"-bines" |
Antimetabolites
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Cancer drugs
"-icins" or "-mycins" |
Antibiotics
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Cancer drugs
"-axel" or "Vin-" |
Microtubulue inhibitors
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Cancer drugs
"-mab" |
Monoclonal antibodies
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Methotrexate
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Antimetabolite
Inhibition of DHF reductase leads to an inhibition of purine ring and dTMP synthesis |
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MECAMYLAMINE
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blocks nicotinic effects
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VARENICLINE
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partial agonist of a2b4 receptor
nicotine replacement and receptor antagonist. Considered the most effective drug for addiction. May lead to suicide. |
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BUPROPION
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Leads to 40% smoking cessation
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NALOXONE
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antagonist which blocks opiate effects
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METHADONE
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slow-acting Full agonist of opiate receptors. Blunt opiate withdrawal – patient remains in normal range without fluctuations between sick / high
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BUPRENORPHINE
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substitute opiate addiction
o Partial agonist – mild agonist activity but prevents opiod from binding – limited euphoric effect, but enough to stop withdrawal symptoms. o Safe medication with fewer side effects. Can be prescribed by physician and used in young people. Reduces negative attitudes associated with Methadone. o Has a “floor effect” on respiratory rate -- does not decrease to ZERO like other opiods |
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DISULFIRAM
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Treatment for alcoholics
Inhibition of Aldehyde dehydrogenase – buildup of acetoaldehyde = unpleasant |
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Protirelin
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Hypothalamic Preparation Used as a Diagnostic Agent in patients with pituitary or hypothalmic dysfunction
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