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147 Cards in this Set
- Front
- Back
Pharmacodynamics
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Is the study of impact of drugs on the body, it includes organ effects, mechanism and adverse effects of drugs
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Pharmacokinetics
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Is a branch dedicated to the determination of the fate of drugs administered externally to a living organism. It deals with ADME
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Absoption
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drug to systemic circulation
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distribution
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drug from systemic circulation to organ
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Elimination
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Through liver and kidney
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Metabolism
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From systemic circulation to liver or kidney
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NSAIDs
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inhibit cycloxygenase 1 and 2, leading to reduction of PGs formation
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Function of ABC exporters (ATP binding cassette)
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expels foreign molecules
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Phase I rxns
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introducing or unmasking a function group to the structure of parent drugs (oxidation, reduction, deamination and hydrolysis)
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Phase II rxns
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conjugation of subgroups to a functional group
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P450
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18 families
43 subfamilies 57 genes |
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Phase II products are water soluble or insoluble
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water soluble
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Potency refers to
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the amount of drug needed to produce an effect. dose to produce 50% of the maximal effect EC50
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Efficacy
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Is defined as potential maximum therapeutic response Emax that a drug causes.
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Emax
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the maximal therapeutic effect caused by a drug
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TD50
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Median toxic dose
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LD50
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median lethal dose
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TI = TD50/ED50
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Therapeutic Index
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5 receptors
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1. Intracelullar(steroid, thyroid)
2. membrane receptors that have enzyme activity(insulin) 3. membrane receptors that bind to tyrosine kinase molecules (cytokines) 4. Membrane receptors that have ion channel function(ACh, GABA, serotonin) 5. Membrane receptor that are coupled with G proteins (DA, NE, 5-HT) |
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Down regulation of receptors
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Caused by agonists
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Up regulation of receptors caused by
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antagonists
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Phase I
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Is it safe? uses volunteers
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Phase II
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Dose it work in patients
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Phase III
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does it work by double blind
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Phase 4
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postmarketing surveillance
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IND
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investigational New Drug
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Criterion as NT
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1. precursor within the presunaptic membrane
2. chemical can be triggered and released by action potentials 3. receptors are located in postsynaptic and presynaptic by action potentials 4. a biochemical inactivation is observed |
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M1
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CNS and glands
contraction of myenteric plexus |
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M2
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Heart, CNS
Decreased heart activity |
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M3
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SM, lungs and glands
Bronchial contraction |
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M4
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CNS
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M5
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Gq protein
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B1
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Heart contractility, stimulates kidney release of renin
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B2
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relaxes SM, but skeletal muscle vessel dilation
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B3
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increases lipolysis
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A1
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SM contraction, glands, stimulates sphincters, increased BP
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A2
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relaxes SM in GI
inhibits secretions, decreased intraocular pressure by blockage of formation of aquous humor |
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Isoproterenol and Dobutamine
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B1 agonists
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Propranolol, Nadolol, Timolol
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nonselective B blockers
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Combined alpha and beta blockers
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Carvedilol and Labetanol
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B2 blocker
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Butoxamine
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B2 agonists
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Albuterol, Epinephrine, NE and Terbutaline
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albuterol, epinephrine, NE and terbutaline
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B2 agonists
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B1 blockers
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Acebutolol, atenolol, esmolol, metoprolol
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Nn
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ANS ganglia
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Nm
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Neuromuscular endplate depolarization
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Muscrine, Pilocarpine and bethanechol
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Muscurinic agonist
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Atropine
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M antagonist
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M1 blockers
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pirenzepine, Dicyclomine
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M2 blocker
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AF-DX116
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N agonists
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Nicotine, varenicline, lobeline
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Nn blocker
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tubocurarine, succinylcholine
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ChE inhibitors
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Neostigmine, physostigmine, parathion, edrophonium
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ChE regenerator compound
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Oxime agents PAM and atropine
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A1 agonist
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Phenylephrine
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A1 blocker
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Prazosin, terazosin, doxazosin, tamsulosin,
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nonselective A blockers
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phentolamine
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Clonidine
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A2 agonist
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A2 antagonist
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yohimbine
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Thiopental has hypoalgesia or hyperalgesia?
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hyperalgesia
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Ketamine blocks what channel?
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glutamate
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What drug has the emergence phenomenon?
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Ketamine
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Local anesthetics block what channel?
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Na+ channel
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Cocaine blocks?
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NE reuptake
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What is the most widely used local anesthetic?
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Lidocaine
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AE's of local anesthetics
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CNS excitation, convulsion, especially with esters
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DOA can be increased by adding a vasoconstrictor or any adrenergic agonist like NE with what type of drugs?
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local anesthetics
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Parkinson's Disease
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damage to DA neurons
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Mesolimbic pathway
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reward and addictive pathway
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Nigrostriatal controls
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voluntary movement
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Strategies to treat PD
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replace DA
Give DA agonist or block DA catabolism |
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DA act at the what receptors?
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D2
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Pramipexole, Ropinerole, Bromocriptine, pergolid, selegiline
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used for PD
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COMT inhibitors
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Tocapone and entacapone for PD
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Huntington's Chorea
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GABAnergic neurons degenerate
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Treatment of HC
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fluoxetine, carbamazepine, tetrabenzepine
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Alzheimer's Disease
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marked atrophy of cerebral cortex, severe degeneration of cholinergic neurons
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AD treatment with cholinesterase inhibitors
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Tacrine, Donepezil, rivastigmine, galantamine, memantidine
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Positive symptoms of Schizophrenia
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hallucination, delusion, disorganized and illogical thought
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Negative symptoms
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flat emotional expressiveness, social isolation or withdrawal
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Is pathogenesis known of schizophrenia?
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no
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Older/typical antipsychotics treat positive or negative symptoms?
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Positive
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Atypical antipsychotics block 5-HT2A or D2 more?
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5-HT2A more
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which atypical antipsychotic can cause agranulocytosis?
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Clozapine
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What are the hypothesis associated with depression?
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Monoamine and neurotropic
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General mechanisms to treat depression are increase synaptic availabiity of:
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NE and serotonin
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SSRI's
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fluoxetine, sertraline, paroxetine
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SNRI's
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venlafaxine, duloxetine and TCA's
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5-HT2 antagonists
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Trazadone
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What are the hypothesis associated with depression?
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Monoamine and neurotropic
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General mechanisms to treat depression are increase synaptic availabiity of:
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NE and serotonin
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SSRI's
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fluoxetine, sertraline, paroxetine
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SNRI's
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venlafaxine, duloxetine and TCA's
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5-HT2 antagonists
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Trazadone
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Tetracyclic and unicyclic antidepressants
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amoxapine, bupropion
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MAOI's
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Phenezine, tranylcypromine
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Mood stabalizing agents
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lithium, carbamazepine, valproic acid
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Constipation is a common side effect with what type of drug?
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opiods
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Naloxone
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opioid antagonist
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Naltrexone, nalmefene
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opioid antagonists
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fentanyl is how many times more potent than morphine?
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100
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What is tetrahydrocannavinoid?
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PHC
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What is the gateway drug?
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Cannavinoids
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Amphotericin B MOA
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binds to ergosterol in the fungal cell membrane, forms channels and increases membrane permeability
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Amphotericin B AEs
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infusion rxns
nephrotoxicity hypokalemia and hypomagnesemia anemia |
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Azole antifungal MOA
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inhibit 14-a-sterol demethylase
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what would you use for aspergillus or candida infection?
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caspofungin only used IV
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caspofungin MOA
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inhibits synthesis of funga cell wall by inhibiting synthesis of B-(1,3)-D-glucan
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Is Flucytosine a prodrug?
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Yes, MOA is 5-FUMP
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Flucytosine AEs
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bone marrow suppression
rash N,V,D elevated LFTs |
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Griseofulvin static or cidal?
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static, inhibits fungal cell mitosis
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Griseofulvin is used for?
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dermatophytic infection
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which drug is similar to Amphotericin B?
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Tolnaftate
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which drug is uses for oral candidiasis?
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Tolnaftate
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What drug causes redness, alopecia, hair discoloration and nail disorders with the lacquer?
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Ciclopirox
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Do Allylamines cause neutropenia?
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Yes
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Isoniazid is cornerstone of treatment for?
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TB
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AEs of Isoniazid?
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Peripheral nuropathy
hepatotoxicity immunologic mediated fever and skin rashes systemic lupus erythematosus-like syndrome |
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Streptomycin is an aminoglycoside, can it be given orally?
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No
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Rifabutin is good for HIV patients bc:
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Less p450 enzyme induction
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What antibiotics can't be used in infants?
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Chloramphenicol
(gray baby syndome) Sulfonamides (kernictirus,bilirubin) |
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What antibiotics can't be used in children?
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Tetracyclines
(teeth discoloration) fuoroquinolones (tendonitis) |
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What antimicrobials can you not drink alcohol with?
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cephalosporins and metrinodazole
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Cell wall active
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bactericidal
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penicillins cidal or static?
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Cidal
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Cephalosporins cidal or static?
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cidal
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Do penicillins have trouble with gram - bacteria?
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Yes bc small peptidoglycan layer
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what generation of cephalosporins cross the BBB?
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3rd and 4th
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carbapenems cidal or static?
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cidal
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what type of administration are carbapenems given?
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only parental administration
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monobactams cidal or static?
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cidal
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vanco broad or narrow?
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Narrow (gram +)
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what antibiotic has red man syndrom and ototoxicity?
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vanco
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Tetracyclines cidal or static?
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static
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Uses of tetracyclines?
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atypical and community acquired pneumonia, chamydia, tularemia from rabbit, rocky mountain spot fever, acne, lyme's PUD and anthrax
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Macrolides cidal or static?
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static
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macrolides broad or narrow?
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broad and atypical coverage
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what is used for treating MAC?
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clarithromycin
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Ketolides broad or narrow?
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narrow
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What is special about quiupristin/Dalfopristin?
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make sure to infuse IV oer at least one hour with D5W and not saline
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Aminoglycosides cidal or static?
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cidal
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aminoglycosides AEs
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otoxicity and neuromuscular blockade
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Quinolones cidal or static?
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cidal
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Sulfonamides cidal or static?
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static
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Polymixin B cidal or static?
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cidal
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Sulfonamides cidal or static?
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static
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Polymixin B cidal or static?
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cidal
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