Term
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Definition
HIV Fusion Inhibitor - by binding gp41 of viral envelope;
Admin SQ, 2X a day;
Met by proteolytic hydrolysis, no CYP rxns;
No cross resistance with OTHER drugs;
Only for tx-experienced pts;
SE - inc risk of bacterial pneumonia |
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Term
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Definition
HIV Fusion Inhibitor - by CCR5 antagonistic activity;
Req CYP3A4 for activity, resistance at P-gp;
Tx R5 HIV serotype ONLY;
SE - cough, rash, dizzy, bladder irritation, liver and cardiac tox |
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Term
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Definition
Nucleoside Reverse Transcriptase Inh (NRTI) - Anti-retroviral;
Nucleoside analog (pyrimidine-T) acts as competitive inhibitor - block elongation in previously uninfected cells;
Req (+P)X3 for axn;
Dec perinatal HIV transmission;
Met by glucaronidation;
Avoid fatty meals (dec AUC);
SE - MYELOSUPPRESSION, lactic acidosis, lipodystrophy |
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Term
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Definition
Nucleoside Reverse Transcriptase Inh (NRTI) - Anti-retroviral;
Nucleoside analog (purine-A,G) forms active ddATP - act as competitive inhibitor - block elongation in previously uninfected cells;
Req (+P)X3 for axn;
Don't take w/ acidic foods (dec AUC);
SE - PERIPHERAL NEUROPATHY, PANCREATITIS, lactic acidosis, lipodystrophy, many drug interaxns |
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Term
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Definition
Nucleoside Reverse Transcriptase Inh (NRTI) - Anti-retroviral, Anti-HBV;
Nucleoside analog (pyrimidine-C) acts as competitive inhibitor - block elongation in previously uninfected cells;
Req (+P)X3 for axn;
Longest NRTI t1/2;
SE - lactic acidosis, lipodystrophy |
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Term
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Definition
Nucleoside Reverse Transcriptase Inh (NRTI) - Anti-retroviral;
Nucleoside analog (pyrimidine-T) acts as competitive inhibitor - block elongation in previously uninfected cells;
Req (+P)X3 for axn;
SE - [worst NTRI] PERIPHERAL NEUROPATHY, PANCREATITIS, lactic acidosis, lipodystrophy, many drug interaxns |
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Term
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Definition
Nucleoside Reverse Transcriptase Inh (NRTI) - Anti-retroviral;
Nucleoside analog (purine-G) acts as competitive inhibitor - block elongation in previously uninfected cells;
Req (+P)X3 for axn;
Met by Alc. Dehydrogenase;
SE - HYPERSENSITIVITY (genetic predisposition), lactic acidosis, lipodystrophy |
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Term
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Definition
Non-Nucleoside Reverse Transcriptase Inh (NNRTI) - Anti-retroviral;
Alosteric binding causes altered active site - inh enzymatic axn;
No HIV-2 axn, (+P) not req;
Hepatic CYP450 met - INDUCER;
Drug interaxn's with PI's;
SE - HEPATOTOX, somnolence, fever, nausea, maculopapular rash; |
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Term
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Definition
Non-Nucleoside Reverse Transcriptase Inh (NNRTI) - Anti-retroviral;
Alosteric binding causes altered active site - inh enzymatic axn;
No HIV-2 axn, (+P) not req;
Hepatic CYP450 met - INHIBITOR;
Drug interaxn's with PI's;
SE - maculopapular rash; |
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Term
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Definition
Non-Nucleoside Reverse Transcriptase Inh (NNRTI) - Anti-retroviral;
Alosteric binding causes altered active site - inh enzymatic axn;
No HIV-2 axn, (+P) not req;
Hepatic CYP450 met - INDUCER;
Drug interaxn's with PI's;
SE - NEUROPSYCHIATRIC, TERATOGENIC, maculopapular rash; |
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Term
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Definition
Nucleotide Inh - Anti-retroviral;
Inhibits reverse transcriptase;
Once daily dosing;
Req ONLY 2 (+P) events;
SE - GI, inc liver enzymes, proximal renal tubulopathy (loss of P and Ca) |
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Term
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Definition
Integrase inhibitor - Anti-retroviral;
Blocks integration of viral (HIV-1!) genome into host genome;
Oral admin, bid;
UGT metabolism (not CYP) by glucaronidation - drug interactions with rifampin, atazanavir; |
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Term
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Definition
Protease inhibitor - Anti-retroviral;
Most eff. ART - competitive, reversible, inh of protease binding site, esp in monocytes, macrophages - blocks MATURATION;
CYP3A4 INHIBITION;
UGT INHIBITION - jaundice;
SE - hyperlipid, DM, lipodystrophy, inc liver enzymes, inc bleeding in hemophliacs; |
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Term
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Definition
Protease inhibitor - Anti-retroviral;
Most eff. ART - competitive, reversible, inh of protease binding site, esp in monocytes, macrophages - blocks MATURATION;
CYP3A4 INHIBITION - but least in class;
LARGE AUC if taken w/ meals;
SE - hyperlipid, DM, lipodystrophy, inc liver enzymes, inc bleeding in hemophliacs; |
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Term
|
Definition
Protease inhibitor - Anti-retroviral;
Most eff. ART - competitive, reversible, inh of protease binding site, esp in monocytes, macrophages - blocks MATURATION;
CYP3A4 INHIBITION - most potent;
SE - HEPATOTOX, hyperlipid, DM, lipodystrophy, inc liver enzymes, inc bleeding in hemophliacs; |
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Term
|
Definition
Protease inhibitor - Anti-retroviral;
Most eff. ART - competitive, reversible, inh of protease binding site, esp in monocytes, macrophages - blocks MATURATION;
CYP3A4 INHIBITION;
SE - hyperlipid, DM, lipodystrophy, inc liver enzymes, inc bleeding in hemophliacs; |
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Term
|
Definition
Protease inhibitor - Anti-retroviral;
Most eff. ART - competitive, reversible, inh of protease binding site, esp in monocytes, macrophages - blocks MATURATION;
CYP3A4 INHIBITION;
SE - ALOPECIA, KIDNEY STONES, LIPODYSTROPHY, hyperlipid, DM, inc liver enzymes, inc bleeding in hemophliacs; |
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Term
|
Definition
Protease inhibitor - Anti-retroviral;
Most eff. ART - competitive, reversible, inh of protease binding site, esp in monocytes, macrophages - blocks MATURATION;
CYP3A4 INHIBITION;
Decent inc in AUC if taken w/ meals;
SE - hyperlipid, DM, lipodystrophy, inc liver enzymes, inc bleeding in hemophliacs; |
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Term
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Definition
Anti-Herpes - Nucleoside analog;
Inh viral DNA pol - chain termination;
Purine analog;
Tx - HSV, VZV, CMV;
Req (+P) by VIRAL thymidine kinase;
SE - HA, nausea, diarrhea, renal, CNS: tremors, delirium, seizures; |
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Term
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Definition
Anti-Herpes - Nucleoside analog;
Inh viral DNA pol - chain termination;
Acyclovir prodrug - Purine analog;
Tx - HSV, VZV, CMV;
Req (+P) by VIRAL thymidine kinase;
SE - HA, nausea, diarrhea, renal, CNS: tremors, delirium, seizures; |
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Term
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Definition
Anti-Herpes - Nucleoside analog;
Inh viral DNA pol - COMPETITIVE INH, NO chain termination;
Penciclovir prodrug - guanine analog;
Tx - HSV, VZV, CMV, also HBV;
Req (+P) by VIRAL thymidine kinase; |
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Term
|
Definition
Anti-Herpes - Nucleoside analog;
Inh viral DNA pol - COMPETITIVE INH, NO chain termination;
Guanine analog;
Tx - HSV, VZV, CMV, also HBV;
Req (+P) by VIRAL thymidine kinase; |
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Term
|
Definition
Anti-Herpes - Nucleoside analog;
Inh viral DNA pol - chain termination;
Tx - CMV DOC, CMV RETINITIS;
Req (+P) by VIRAL thymidine kinase;
100X more potent than Acyclovir;
SE - MYELOSUPP., TERATOGENIC, HA, nausea, diarrhea; |
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Term
|
Definition
Anti-Herpes - Nucleoside analog;
Inh viral DNA pol - chain termination;
Prodrug of Ganciclovir, req hydrolyzation by esterases;
Tx - CMV DOC, CMV RETINITIS;
Req (+P) by thymidine kinase;
100X more potent than Acyclovir;
SE - MYELOSUPP., TERATOGENIC, HA, nausea, diarrhea; |
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Term
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Definition
Anti-Herpes - NucleoTIDE analog;
No (+P) by viral TK;
Tx - HSV, VZV, CMV RETINITIS;
SE - NEPHROTOX, neutropenia, carcinogenic, ocular hypotony |
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Term
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Definition
Pyrophosphate analog - Anti-Herpes;
"Non-nucleoside";
Inh DNA pol by blocking cleavage, ALSO Inh HIV-RT;
NO (+P) required;
Tx - nucleoside resistant cases (HSV, VZV, CMV), CMV retinitis;
SE - NEPHROTOX, N/V, anemia, fatigue |
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Term
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Definition
Anti-hep - Nucleotide (A) analog;
Inhibits HBV DNA pol - tx HBV;
No cross resisitance w/ Lamivudine;
SE - rebound hep, nephrotox, lactic acidosis and hepatomegaly |
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Term
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Definition
Anti-viral, anti-immune, anti-prolif;
Activates Jak-Stat;
Inh viral entry, transciption, uncoating, and viral protein synth;
Tx - HBV, HCV, HPV, HHV-8 (kaposi sarc);
SE - myelosupp, N/V, neurotox, inc creatinine, proteinuria |
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Term
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Definition
Anti-hep - nucleoside analog (G);
Competitive inh of GTP 5' capping of viral mRNA;
Concentrates in RBCs;
Tx - HCV, RSV;
SE - hemolytic anemia, teratogenic, myelosupp. |
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Term
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Definition
Anti-Parkinsonism, Anti-flu - Uncoating inh;
Blocks HA glycoprotein maturation - blocks binding to M2 ion channel;
No internal acidification;
Work on Flu-A ONLY;
Enhances DA release;
"Good alternative to flu vaccine";
SE - restless, depression, psychosis, hallucinations, confusion;
CI - seizures, heart failure |
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Term
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Definition
Anti-flu - Uncoating inh;
Blocks HA glycoprotein maturation - blocks binding to M2 ion channel;
No internal acidification;
Work on Flu-A ONLY;
"Good alternative to vaccine"; |
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Term
|
Definition
Anti-flu - Viral Release Inh;
Inh viral neuraminidase - no cleavage of sialic acid - destroys receptors recognized by HA - no detachment from host cell;
Admin via inhalation (low PO bioavail);
Tx flu-A(2nd line) and B |
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Term
|
Definition
Anti-flu - Viral Release Inh;
Inh viral neuraminidase - no cleavage of sialic acid - destroys receptors recognized by HA - no detachment from host cell;
Tx flu-A(2nd line) and B |
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Term
| Chloropromazine (Thorazine) |
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Definition
Typical Anti-Psychotic - low potency;
Inh of D2 receptor - effective for positive symptoms;
Aliphatic side chain - low potency (dec risk of EPS, inc risk of anti-muscarinic effects);
Tx for Huntington's chorea(DA antagonism;
SE - corneal deposits, INC PRL (severe), DEC INSULIN, JAUNDICE, ANTI-DIURETIC, ORTHOSTATIC hypoT, skin rxns, EPS |
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Term
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Definition
Typical Anti-Psychotic - hi potency;
Inh of D2 receptor - effective for positive symptoms;
Piperazine group - inc potency (inc risk of EPS, dec anti-muscarinic effects);
SE - EPS, inc PRL, skin rxns |
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Term
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Definition
Typical Anti-Psychotic;
Inh of D2 receptor - effective for positive symptoms;
Piperdine ring;
Dec incidence of EPS;
SE - inc PRL, highly anti-muscarinic |
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Term
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Definition
Typical Anti-Psychotic - hi potency;
Inh of D2 receptor - effective for positive symptoms;
Tx for Huntington's chorea(DA antagonism);
SE - EPS, inc PRL |
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Term
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Definition
Atypical Anti-Psychotic;
D2 and 5-HT2 (high affinity) antagonism;
Inc efficacy for Negative symptoms (as well as positives);
Limited EPS;
SE - BLOOD DYSCRASIAS (esp leukopenia) inc risk of DM typeII, weight gain; |
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Term
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Definition
Atypical Anti-Psychotic;
D2 and 5-HT2 (high affinity) antagonism;
Inc efficacy for Negative symptoms (as well as positives);
Tx CHILDREN AND TEENS;
Limited EPS;
SE - inc risk of DM typeII, metabolic syndrome; |
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Term
|
Definition
Atypical Anti-Psychotic;
D2 and 5-HT2 (high affinity) antagonism;
Inc efficacy for Negative symptoms (as well as positives);
SE - WEIGHT GAIN, METABOLIC SYNDROME (hi incidence), inc risk of DM typeII; |
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Term
|
Definition
Atypical Anti-Psychotic;
D2 and 5-HT2 (high affinity) antagonism;
Inc efficacy for Negative symptoms (as well as positives);
No effect on PRL levels;
SE - METABOLIC SYNDROME, inc risk of DM typeII; |
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Term
|
Definition
Atypical Anti-Psychotic;
D2 and 5-HT2A,1A,2C (high affinity) antagonism;
Inc efficacy for Negative symptoms (as well as positives);
Limited EPS;
SE - inc risk of DM typeII; |
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Term
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Definition
Atypical Anti-Psychotic;
D2 partial agonist, 5-HT2 antagonist, and 5-HT1A partial agonist;
Inc efficacy for Negative symptoms (as well as positives);
No effect on PRL levels;
SE - inc risk of DM typeII; |
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Term
| CNS effects of Anti-Psychotics (6 sites) |
|
Definition
Cortex - dec seizure threshold;
Basal ganglia - inc DA metabolism, inc Ach turnover;
Limbic - main site of anti-psychotic efx;
Hypothalamus - inc PRL;
Brainstem - dec reflexes;
CTZ - protect AGAINST N/V |
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Term
| Endocrine effects of Anti-Psychotics |
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Definition
|
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Term
| Cardiovascular effects of Anti-Psychotics |
|
Definition
Direct and indirect effects;
Orthostatic hypotension - esp chlorpromazine |
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Term
| EPS of of Anti-Psychotics (6) |
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Definition
Acute dystonia;
Akathesia;
Parkinsonian syndrome;
Neuroleptic Malignant Syndrome;
Perioral tremor;
Tardive dyskinesia |
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Term
| Anti-cholinergic effects of Anti-Psychotics |
|
Definition
Dry mouth;
blurred vision;
constipation;
nasal congestion;
orthostatic hypoT |
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Term
|
Definition
Parkinsonism Tx;
Allowed to cross BBB and Conv to DA by endogenous L-AAD @CNS AND peripherally (large dose req'd);
First line for Park. but can only use 3-5 years;
SE - anorexia, orthostatic hypoT, arrhythmias (Afib), tachycardia;
CI - Vit B6, MAOI, glaucoma, psychosis, ulcers CV dz |
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Term
| L-DOPA/carbidopa (Sinemet) |
|
Definition
Parkinsonism Tx;
L-DOPA fxn PLUS...
Peripheral inh of L-AAD - dec amt of L-DOPA req for therapy;
Fluctuating responses;
SE - depression, anxiety, delusions, chorea, tics;
CI - Vit B6, MAOI, glaucoma, psychosis, ulcers CV dz |
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Term
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Definition
Parkinsonism Tx - DA receptor agonist;
Activate D2 - dec activation of indirect basal ganglia pathways;
D2 agonist, D1 partial agonist;
Tx EARLY dz |
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Term
|
Definition
Parkinsonism Tx - DA receptor agonist;
Activate D2 - dec activation of indirect basal ganglia pathways;
D1/D2 agonist, inc efficacy;
Tx EARLY dz |
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Term
|
Definition
Parkinsonism Tx - DA receptor agonist;
Activate D2 - dec activation of indirect basal ganglia pathways;
D2 selective agonist;
Tx EARLY dz |
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Term
|
Definition
Parkinsonism Tx - DA receptor agonist;
Activate D2 - dec activation of indirect basal ganglia pathways;
D2 selective agonist;
CYP1A2 met;
Tx EARLY dz |
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Term
|
Definition
Parkinsonism Tx - MAO-B inhibitor;
Dec breakdown of DA;
Metabolites will inc DA release;
Dec free radical production from MAO-B;
CI - TCAs, SSRIs, meperidine |
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Term
|
Definition
Parkinsonism Tx - MAO-B inhibitor;
Dec breakdown of DA;
INC POTENCY;
2nd line tx |
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Term
|
Definition
Parkinsonism Tx - COMT inhibitor;
Prolong axn of L-DOPA and dec it's transport-competitor 3OMD;
PERIPHERAL AXN;
Preferred due to dec SE's |
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Term
|
Definition
Parkinsonism Tx - COMT inhibitor;
Prolong axn of L-DOPA and dec it's transport-competitor 3OMD;
PERIPHERAL AND CENTRAL AXNS;
SE - hepatotox |
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Term
|
Definition
Parkinsonism Tx - Anti-muscarinic;
Alter DA/Ach balance by blocking Ach-stimulation of striatum;
Tx early Park or as adjunct to L-DOPA;
SE - drowsy, inattention, delusions, hallucinations, typical ANS anti-Ach axns |
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Term
| Diphenhydramine (Benadryl) |
|
Definition
Parkinsonism Tx - Anti-muscarinic;
Alter DA/Ach balance by blocking Ach-stimulation of striatum;
Tx early Park or as adjunct to L-DOPA;
SE - drowsy, inattention, delusions, hallucinations, typical ANS anti-Ach axns |
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Term
|
Definition
Parkinsonism Tx - Anti-muscarinic;
Alter DA/Ach balance by blocking Ach-stimulation of striatum;
Tx early Park or as adjunct to L-DOPA;
SE - drowsy, inattention, delusions, hallucinations, typical ANS anti-Ach axns |
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Term
|
Definition
Alzheimer's Dz Tx - Ach-esterase Inh;
Inc lvls of Ach;
DEC USE due to dec bioavail, inc SE, hi protein binding;
SE - HEPATOTOX, GI, insomnia, bradycardia |
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Term
|
Definition
Alzheimer's Dz Tx - Ach-esterase Inh;
Inc lvls of Ach;
Long t1/2 - 70hrs;
SE - GI, insomnia, bradycardia |
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Term
|
Definition
Alzheimer's Dz Tx - Ach-esterase Inh;
Inc lvls of Ach;
Short t1/2;
SE - GI, insomnia, bradycardia |
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Term
|
Definition
Alzheimer's Dz Tx - Ach-esterase Inh;
Inc lvls of Ach;
SE - GI, insomnia, bradycardia |
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Term
|
Definition
Alzheimer's Dz Tx;
Blocks NMDA-type glutamate receptors - dec glutamate axn;
Also blocks 5-HT3 and Ach-R;
Allows for physiologic Glu axn w/out the dmg from high lvls;
Slow's dz progression;
SE - confusion, HA, insomnia, agitation, hallucination, hypertonia, cystitis, inc libido |
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Term
|
Definition
SSRI - inhibits SERT to potentiate serotonin action;
Tx depression typically assoc w/ Huntington's |
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Term
|
Definition
inhibits DA and NE movement into synaptic vesicles;
Depletes CNS dopamine stores;
Tx Chorea assoc w/ Huntington's |
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Term
|
Definition
ALS tx;
Dec Glu release by (1) block inactive Na-channel, (2) block activated Ca-channel;
Also (3) block NMDA channel;
Met by CYP1A2;
Hi protein binding;
SE - fatigue, sedation, liver dz |
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Term
| Interferon beta-1a (Avonex)(Rebif) |
|
Definition
MS tx - Anti-inflamm;
Restores BBB - dec immune response in CNS;
SC admin;
Tx - remitting-relapsing MS, effective in 30%;
SE - depression, hepatotox, miscarriage, immunosup |
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Term
|
Definition
MS tx - Anti-inflamm;
Restores BBB - dec immune response in CNS;
More effective than interferon;
Tx also Crohn's;
SE - PML!! (progressive multifocal leukoencephalopathy) |
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Term
|
Definition
MS tx - myelin decoy;
Tx - remitting-relapsing MS;
SE - Injxn site rxns, incl lipoatrophy |
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Term
|
Definition
MS tx - anti-neoplastic;
Topo-II inhibitor;
Tx - secondary progressive MS |
|
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Term
|
Definition
MS tx - anti-neoplastic;
Monoclonal Ab against CD52 on T-cells |
|
|
Term
| 4-AP (Dalframpridine)(Ampyra) |
|
Definition
MS tx - new!;
Blocks Shaker K channel and potentiates Ca channel - prolong AP duration and enhance NT release;
Tx - improves walking speed |
|
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Term
|
Definition
MS tx - new!;
Activation of S1PR (G-protein coupled) - retains lymphcytes in the lymph node - dec auto-immune rxn against myelin!;
Tx - reduce relapses and dz progression in relapsing forms; |
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Term
|
Definition
Anti-Epilepsy - Hydantoin;
Stabilizes inactive Na channels;
Met by CYP2C4, induces 2C and 3A;
Highly protein bound - competes w/ other drugs (warfarin, OCT, carbamazepine);
SE - [narrow TI] nystagmus, ataxia, arrhythmias, coarsened face, hirsutism, gingival hyperplasia, peripheral neuropathy, bone disruption, teratogenic |
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Term
|
Definition
Anti-epilepsy - barbiturate;
Prolong opening of GABA receptor;
Blocks AMPA receptor;
Induce CYP2b6 and UGT;
SE - sedation, lethargy, nystagmus, rash, megaloblastic anemia, dec vitD |
|
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Term
|
Definition
Anti-epilepsy - iminostilbenes;
Mood-stabilizer;
Prolongs Na channel recovery;
Met by CYP2C9,3A4 to active 10,11-epoxide;
Induces CYP1A2, 2B6, 2C19, UGT;
Tx - DOC for partial seizures, T/C, mood stabilizer for bipolar, trigeminal neuralgia;
Tx depression typically assoc w/ Huntington's;
SE - blood dyscrasias, diplopia, ataxia |
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Term
|
Definition
Anti-epilepsy - succinimides;
Inh of T-type Ca channels - prevents 3Hz spike/waves;
Inc AUC when given w/ valproic acid;
Met by hydroxylation;
Tx - DOC for absence seizures;
SE - [tolerance] euphoria, hiccups, fatigue |
|
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Term
|
Definition
Anti-epileptics - Carboxyllic acid;
Stabalizes inactive Na channels, Dec Ca current, stimulates GABA synth and inhibits degradation;
Met by UGT via beta-ox - also inhibits it;
Inh CYP2C9;
Tx - absence + T/C DOC, myoclonic, partial;
Inc [plasma] phenobarb, phenytoin, carbamazepine;
SE - heartburn, liver tox, teratogenic; |
|
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Term
|
Definition
Anti-epilepsy - BNZ;
Inc opening of GABA Cl channel;
Can be given rectally;
Tx - refractory myoclonic, atonic, absence;
SE - sedation, lethargy |
|
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Term
|
Definition
Anti-epilepsy - BNZ;
Inc opening of GABA Cl channel;
Tx - DOC status epilepticus;
SE - sedation, lethargy |
|
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Term
|
Definition
Anti-epilepsy - BNZ;
Inc opening of GABA Cl channel;
Long acting, can admin rectally;
Tx - status epilepticus;
SE - sedation, lethargy |
|
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Term
|
Definition
Anti-epilepsy;
Structural analog of GABA, and may inc GABA release;
Tx - [adjunct] partial, neuropathic pain, neuralgia;
SE - somnolence, ataxia |
|
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Term
|
Definition
Anti-epilepsy;
Delays recovery of inactivated Na channels;
Tx - [adjunct] partial, T/C, absence;
SE - visual, rash, SJS |
|
|
Term
|
Definition
Anti-epilepsy;
MOA not understood;
Tx - [adjunct] T/C, myoclonic;
SE - dizzy, somnolence |
|
|
Term
|
Definition
Anti-epileptics;
Inh voltage Na channels, inc GABA axn, inh AMPA receptors;
Tx - partial +/- T/C seizures;
SE - CA inhibition to make kidney stones |
|
|
Term
|
Definition
Anti-epileptic;
Inh NMDA-evoked responses, inc GABA axn;
Tx - [adjunct] partial and secondary generalizes seizures;
SE - aplastic anemia |
|
|
Term
|
Definition
Anti-epileptic;
Inh Na channels, inh T-type Ca channels;
Tx - parital seizures, infantile spasm, myoclonic, generalized and absence;
Met by CYP3A4; |
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