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Pharm Block 2 pt. 2

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alex0624's version from 2016-06-30 01:14

Hypolipidemics

Question Answer
↓Cholesterol synthesis (on liver cells)Statins
Competitive inhibitors of HMG-CoA reductaseStatins
↑LDL receptor, thus lowering serum LDL levels.Statins
Side effect; Hepatotoxicity (↑AST/ALT), myopathy (muscle pain)Statins
Due to toxicity of this drug AST/ALT & Creatine Kinase must be monitoredStatins
↓ Synthesis of VLDL & TG levelsNiacin (Nicotinic Acid)/Vit. B3
Side effect; Flushing, diarrhea, hepatic dysfunction, nausea, pruritus, goutNiacin (Nicotinic Acid)/Vit. B3
Treatment for Niacin toxicityNSAIDs
↑Lipoprotein Lipase (LPL)Gemfibrozil and Fenofibrate (Fibrates -PPARα agonist)
Peroxisome proliferator-activated receptor α (PPARα) agonistGemfibrozil and Fenofibrate
Fibric Acid DerivativesGemfibrozil and Fenofibrate
Side effects; GI symptoms, myopathy, risk of cholesterol gallstones.Gemfibrozil and Fenofibrate
Typically used to treat hypertriglyceridemia.Gemfibrozil and Fenofibrate
Major drug interaction; displace warfarin and sulfonyl ureas (anti diabetic drug)Gemfibrozil and Fenofibrate
Interrupts enterohepatic circulation of bile acids, ↑Synthesis of bile acids, ↑Synthesis of LDL receptorsColestipol, Cholestyramine and Colesevelam
Side effects; Bad taste, constipation, bloating, nausea, fat soluble vitamin deficiencyColestipol, Cholestyramine and Colesevelam
↓ Intestinal absorption of cholesterol (lowers LDL & TG)Ezetimibe
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Eicosanoids

Question Answer
Histamine receptor found on blood vessels(smooth muscle, and bronchus)H1 (Gq-↑ IP3 and DAG)
Histamine receptor that causes Vasodilation - ↓ BP (by releasing NO)(H1) Gq-↑ IP3 and DAG
Histamine receptor found on Stomach (parietal cells)H2 (Gs- ↑cAMP)
Histamine receptor that stimulates gastric secretionH2 (Gs- ↑cAMP)
Histamine drugs with the following effects; Sedation, Peripheral antimuscarinic actions (alpha blocking-postural hypertension). Central antimuscarinic actions (which leads to its use in treating drug induced Extra Pyramidal Symptoms)Diphenhydramine, Chlorpheniramine, Promethazine, Hydroxyzine (H1 antagonist, 1st generation drugs causing sedation)
Diphenhydramine(benadryl)H1 antagonist, 1st generation drugs causing sedation
ChlorpheniramineH1 antagonist, 1st generation drugs causing sedation
PromethazineH1 antagonist, 1st generation drugs causing sedation
HydroxyzineH1 antagonist, 1st generation drugs causing sedation
Loratidine, Fexofenadine, cetirizine2nd generation(non sedating)
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Metabolite of fentenadine: Fexofenadine
Question Answer
Two types of drugs used in motion sicknessH1 blockers and Scopalamine (M & H1 blocker)
Competitive (antagonist) blockade of H2-receptorsCimetidine, Ranitidine, Famotidine
H2 Receptor antagonists that inhibits CYP450 & blocks androgen receptorsCimetidine
Marker of carcinoid syndrome5HIAA
Treatment for flushing, diarrhea, bronchoconstriction (carcinoid syndrome)Octreotide
5HT1-A locationRaphe nuclei (anxiety)
5HT1-B locationStriatum, substantia nigra
5HT1-D locationCranial blood vessels (migranes)
5 HT1-B/D agonistSumatriptan
Rx for acute migraine attackSumatriptan
activation of 5HT1-B/D agonist, inhibit the activation of the trigeminal nerve anthis eeffect inhibits meningeal vasodilationSumatriptan
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Produce meningeal vasoconstricition :Sumatriptan
Question Answer
5HT1A agonistBuspirone
Rx for General Anxiety DisorderBuspirone
5 HT2 & alpha adrenoceptor blockerKetanserine
Rx of schizophreniaOlanzapine
5HT2a antagonistOlanzapine
Used in carcinoid tumors - 5HT2 antagonistCyproheptadine
Control of vomiting associated with chemotherapyOndansetron
5 HT3 receptor antagonistsOndansetron
Use in obstetric bleeding- post partum haemorrhage (stimulate uterine contraction)Ergonovine (preferred) & Ergotamine
Ergot Rx for Hyperprolactinemia & ParkinsonBromocriptine, pergolide (both Dopamine Agonist)
Ergot Rx for Parkinson’s diseaseBromocriptine
Ergot Rx for Carcinoid tumourMethysergide
Ergot Rx for Acute attack of migraineErgotamine
Prevents recurrent migrane episodesPropanolol
Prevents recurrent migraine episodesSodium valproate
Type of natural Prostaglandin that keeps the Ductus arteriosus (DA) open in fetusPGE2
Rx to close Ductus Arteriosus Indomethacin (NSAID)
Rx for Dysmenorrhea; Excessive pain (usually crampy) during mensesNSAIDs (ibuprofen)
Mechanism of Nitric Oxide (NO)Increased cGMP levels
The only approved used of Nitric Oxide (NO)Pulmonary artery hypertension and acute respiratory distress syndrome in neonates - Given by inhalation
↑ cGMP by inhibiting its breakdown by phosphodiesterase isoform 5 (inhibitor)Sildenafil (viagra)
Side effects on color vision, causing difficulty in blue-green discriminationSildenafil
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Prostaglandins (Eicosanoids)

 

Question Answer
PGE1 drug used to maintain the patency of Ductus ArteriosusAlprostadil (Vasodilation)
PGE1 drug used to treat erectile dysfunctionAlprostadil (Vasodilation)
PGE1 used in treatment of NSAID induced peptic ulcers. Gastric cytoprotectionMisoprostol
Misoprostol (PGE 1) with mifepristone (antiprogestin) are used toInduce abortions
PGE2 used in ‘cervical ripening’ and as abortifacient (Contraction of uterine muscle)Dinoprostone
PGF2α used in ‘cervical ripening’ and as abortifacient and postpartum bleeding (Contraction of uterine muscle)Carboprost
Causes Dysmenorrhea; Excessive pain (usually crampy) during mensesPGE2 and PGF2α
PGF2α used as Rx for glaucomaLatanoprost
Increases the out flow of aqueous humor from anterior chamber of the eye, reducing intraoccular pressureLatanoprost
PGI2 Used in pulmonary hypertensionEpoprostenol (Vasodilation)
AlprostadilPGE1 Maintains PDA open)
CarboprostPGF2α
DinoprostonePGE2
EpoprostenolPGI2
LatanoprostPGF2α
MisoprostolPGE1(usde in treatment of NSAID- induced peptic ulcer)
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Sedative Hypnotics

Question Answer
Benzodiazepines antagonistFlumazenil
How does the body get rid of Phenobarbital and other barbituatesAlkalinization of the urine
Bind to BZ1 receptor, on GABA-ABenzodiazepines
Increased frequency of chloride channel openings causing hypo polarization and CNS depressionBenzodiazepines
Act on GABA-A receptor complex . Causes prolong duration of chloride channel openings causing hypo polarization and CNS depressionBarbiturates
Barbiturate with the shortest half life. Rapid onset of action (enters CNS fast)Thiopentone
Benzodiazepine with the shortest half life. Rapid onset of action (enters CNS fast)Triazolam & Alprazolam
Benzodiazepine with the longest half lifeChlordiazepoxide, Diazepam, Prazepam, and Clorazepate
Exert dose-dependent anterograde amnesic effects (inability to remember events occurring during the drug's duration of action)Benzodiazepines
DOC for Status EpilepticusDiazepam
Effective at sedative dose levels for specific spasticity states. Mechanism: by inhibiting spinal reflexes, causes Skeletal muscle relaxationDiazepam
DOC for febrile convulsionsDiazepam
DOC for chronic alcohol withdrawalDiazepam
DOC for Panic disorders and some phobias (Agoraphobia)Alprazolam or clonazepam
DOC for Preanesthetic medication, IV General AnesthesiaMidazolam
DOC for insomniaTriazolam
Drugs that is Safer in old age patients with insomnia because they do not form active metabolites. Also safer in those with hepatic diseasesOxazepam and lorazepam
Used for Date RapeFlunitrazepam
DOC for Acute Anxiety DisordersPropranolol (fast acting)
DOC for Obsessive-Compulsive Disorder (OCD)Clomipramine
DOC for Generalized Anxiety Disorder (GAD)Buspirone
Barbiturates used for seizuresPhenobarbitone
Barbiturates used for induction of anesthesiaThiopental
Contraindicated in BZD abusive mother as it increases risk for seizures in newbornFlumazenil
Acts as a partial agonist on 5-HT1A autoreceptors . Takes 1 to 2 weeks for effectsBuspirone
Agonist at MT1 and MT2 melatonin receptors. Used in management of insomniaRamelteon
Zolpidem and Zaleplon their effects are antagonized byFlumazenil
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Antiepileptics

Question Answer
Antiepileptics that blocks Na channels firing at high frequenciesCarbamazepine, Phenytoin, Valproate, Phenobarbitone(high concentrations affect Cl and Na)
GABA transaminase inhibitors (metabolize GABA)Valproate (valproic acid) & Vigabatrin
What would be the effect on the membrane of increasing Cl- influx during a seizure?Hyperpolarization *which decreases seizure activity*
Antiepileptic drugs that inhibits the breakdown of γ-aminobutyric acid (GABA) by acting as a suicide inhibitor of GABA transaminase (GABA-T)Valproate (valproic acid) & Vigabatrin
Structural analogue of the inhibitory neurotransmitter γ-aminobutyric acid (GABA)Gabapentin
Prolong duration of GABA-mediated chloride channel openingsBarbiturates
Increase frequency of GABA- mediated chloride channel openingsBenzodiazepines
Open Cl- channel (by Enhancing GABA transmission). Blocks voltage-dependent sodium channels. Blocks T-type calcium currents (Thalamic neurons)Valproate
Reduction in the flow of Ca++ through T-type Ca++ channels in thalamusEthosuximide & Valproate
DOC in absense seizuresEthosuximide & Valproate
Bind to presynaptic voltage gated N type of Ca2+channel - ↓ synaptic release of glutamateGabapentin, Pregbalin
Irreversibly inhibits GABA transaminase (GTA)Vigabatrin
Bind to synaptic vesicular protein (SV2A) – ↓ synaptic release of glutamateLevetiracetam
Antiepileptic drug that is protein bound, CYP enzyme inducer and follows zero order kinetics (constant amount is eliminated)Phenytoin
Antiepileptic drug that is plasma protein bound and is a CYP enzymes inhibitorValproic acid
Antiepileptic drugs that are CYP enzymes inducersCarbamazepine, phenobarbitone, phenytoin
Drug that causes Gingival HyperplasiaPhenytoin
Antiepileptic side effects: diploplia, ataxia, hyponatremia (↑ADH) , teratogenic (cleft lip and palate)Carbamazepine
Antiepileptic side effects: Hepatotoxicity (children), Spina bifida. Weigth gain.Valproic acid
Benzodiazepans used for seizuresdiazepam, clonazepam, lorazepam, Nitrazepam
Increase in Cl infflux in CNS cause?Hyperpolarization
Gabapentin, Pregbalinbind to presynaptic voltage gated N type of Ca2+channel - decrease synaptic release of glutamate
Vigabatrinirrevrisibly inhibits GABA transaminase (GTA)
Lamotrigineprolongs inactivation of Na channels, presynaptic voltage gated N type of Ca2+channel - decrease synaptic release of glutamate
Tiagabineblock GABA reuptake by blockade of GAT (GABA transporter)
Levetiracetambind to synaptic vesicular protein (SV2A) – decrease synaptic release of glutamate
Felbamateblock NMDA (glutamate) receptors
CYP enzyme inhibitorValproic acid
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Drug interaction of Pheytoin and valproic acid :Displace warfarin and sulfonamides

 

Question Answer
DOC inmmediate in Status epilepticus(repetitive GCT seizures)inmediate Diazepam IV or lorazepam IV
DOC maintainance in status epilepticusPhenytoin(IV) and Phenobarbitone(IV)
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DOC for GTC and partial seizures Carbamezipane, Valproate, Phenytoin phenobarbitones
Question Answer
DOC in abscence seizuresValproate and ethosuximide
DOC in complete partial seizuresCarabamezipane, Valproate and phenytoin.
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DOC for Febrile convulsions: diazepam
Question Answer
DOC for Myoclonic seizuresvalproic acid, zonisamide,
DOC for Status epilepticusdiazepam, lorazepam, phenytoin
Carbamazepine used fortrigeminal neuralgia
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Bipolar disorder: valproic acid, carbamazepine.