AIIMS---DRUGS--PHARM---a drug in a post for aiims

Discussion in 'AIIMS Nov 2013' started by samuel, Aug 21, 2014.

  1. samuel

    samuel New Member

    RANOLAZINE--500 to 1000mg twice daily

    piperazine derivative
    may be useful for patients with chronic angina despite standard
    medical therapy
    inhibition of the late inward sodium current (I Na )
    contraindicated in patients with
    1.hepatic impairment
    2.conditions or drugs associated withQT c prolongation
    3.drugs that inhibit the CYP3A metabolic system
    another minor MOA--pFOX inhibition (fatty acid oxidation) shift away from fatty acid metabolism
  2. samuel

    samuel New Member

    ETHOSUXIMIDE-Therapeutic levels of 60–100 mcg/mL (750–1500 mg/d)

    blocks T type calcium channels(T-type calcium currents are thought to provide a pacemaker current in thalamic neurons responsible for generating the rhythmic cortical discharge of an absence attack)

    not protein-bound
    completely metabolised by hydroxylation
    mc dose related adverse effect -gastric distress
    t1/2---40 hrs

    absence seizures
  3. samuel

    samuel New Member

    IRINOTECAN(pro drug)(carboxylesterase enzyme converts it to active metabolite)

    potent inhibitor of topoisomerase I
    eliminated via bile(in contrast to topotecan which is eliminated in urine so dose reduction in renal impairment)
    second-line monotherapy in patients with metastatic colorectal cancer who had failed fluorouracil-based therapy(1st line when used with 5FU and leucovorin)
    early form(<24 hrs) of diarrhea--due to cholinergic stimulation(anticholinergics are the treatment)
  4. samuel

    samuel New Member

    BUSPIRONE---anxiolytic--- partial agonist at brain 5-HT1A receptors

    no anticonvulsant or muscle relaxant properties
    no rebound anxiety or withdrawal signs on abrupt discontinuance
    unsuitable for management of acute anxiety states
    extensive first-pass metabolism via hydroxylation and dealkylation reactions
    elimination half-life of buspirone ---2–4 hours
    Buspirone causes less psychomotor impairment than benzodiazepines

    Tachycardia, palpitations, nervousness, gastrointestinal distress, and paresthesias and a dose-dependent pupillary constriction
  5. samuel

    samuel New Member

    BUPROPION---Anti depressant--norepinephrine-dopamine reuptake inhibitor (NDRI)

    non-tricyclic antidepressant
    does not cause sexual dysfunction(unlike many other anti-depressant)

    useful in depression,Seasonal affective disorder,smoking cessation

    Dizziness, dry mouth, sweating, tremor, aggravation of psychosis, potential for seizures at high doses

    CI: epileptics
  6. samuel

    samuel New Member

    BRETYLIUM---class 3 anti arrhythmic

    ------Since bretylium causes an initial release of catecholamines, it has some positive inotropic actions when first administered. This action may also precipitate ventricular arrhythmias and must be watched for at the onset of therapy with the drug.

    ----lengthens the ventricular (but not the atrial) action potential duration and effective refractory period

    ----may result in postural hypotension
  7. samuel

    samuel New Member

    cycloserine,penicillamine,INH,hydralazine interferes with PYRIDIXINE metabolism

    INH---inhibits synthesis of mycolic acids---5 mg/kg in children

    -active against both extracellular and intracellular organisms
    -prodrug that is activated by KatG, the mycobacterial catalase-peroxidase
    -acetylation by liver N-acetyltransferase
    -dose need not be adjusted in renal failure
    -isoniazid is contraindicated if it is the cause of the hepatitis

    -Peripheral neuropathy is observed in 10–20% of patients given dosages greater than 5 mg/kg/d but is infrequently seen with the standard 300 mg adult dose
    -Isoniazid-induced hepatitis is the most common major toxic effect(risk of hepatitis depends on age)

    -Isoniazid can reduce the metabolism of phenytoin, increasing its blood level and toxicity.
  8. samuel

    samuel New Member

    MIRABEGRON----BETA3 adrenergic agonist

    -used in overactive bladder(relaxes detrusor and increases bladder capacity)

    -C/I : ESRD
    severe hepatic impairment

    -ADR: elevation of BP(especially in pre existing HT)
    dry mouth
  9. samuel

    samuel New Member

    BEVIRIMAT-maturation inhibitor for HIV

    similar to protease inhibitor in action as it prevents maturation

    interferes with processing of GAG
  10. samuel

    samuel New Member

    BIPYRIDINES----PDE-3 inhibitor

    inamrinone & milrinone
    effective orally and parenterally but only parenteral prep available
    t1/2 3 to 6 hrs 10 to 40% excreted in urine

    1.The bipyridines increase myocardial contractility by increasing inward calcium flux in the heart during the action potential

    2.have an important vasodilating effect. Inhibition of phosphodiesterase results in an increase in cAMP and the increase in contractility and vasodilation.

    only for acute heart failure or for severe exacerbation of chronic heart failure.

    nausea and vomiting; arrhythmias, thrombocytopenia, and liver enzyme changes(less seen in milrinone)
  11. samuel

    samuel New Member

    FDA approves inhaled form of insulin
    Afrezza Inhalation Powder

    The FDA approved Afrezza with a boxed warning – the strongest type – indicating that the drug should not be used in patients with chronic lung diseases, such as asthma and smoker's cough, due to reports of breathing spasms.

    ultra rapid acting form of inhalable insulin with peak plasma concentrations that mimic physiologic mealtime response at 12–14 minutes(not a substitute for long-acting insulin.)

    is intended to be used in combination with long-acting insulin for patients with type 1 diabetes, the FDA said
  12. samuel

    samuel New Member

    ACUTE ATTACKS OR INITIAL DEMYELINATING EPISODES(after excluding pseudo exacerbations)---glucocorticoids

    (1) IFN-β-1a
    (2) IFN-β-1a
    (3) IFN-β-1b
    (IFN-Beta----immunomodulatory properties, including (1) downregulating
    expression of MHC molecules on antigen-presenting cells,
    (2) inhibiting proinflammatory and increasing regulatory
    cytokine levels, (3) inhibition of T cell proliferation, and
    (4) limiting the trafficking of inflammatory cells in the CNS)

    (4) glatiramer acetate ---synthetic, random
    polypeptide composed of four amino acids (l-glutamic acid,
    l-lysine, l-alanine, and l-tyrosine)

    (MOA-(1) induction of antigen-specific suppressor
    T cells; (2) binding to MHC molecules, thereby displacing bound
    MBP; or (3) altering the balance between proinflammatory and
    regulatory cytokines)
    (5) natalizumab---against the α 4 subunit of α 4 β 1 integrin
    (lymphocytes from binding to endothelial cells,
    thereby preventing lymphocytes from penetrating the BBB and
    entering the CNS)
    (6) fingolimod ---sphingosine-1-phosphate
    (S1P) inhibitor
    MOA-prevents the egress of lymphocytes
    from the secondary lymphoid organs such as the lymph nodes
    and spleen
    (7) mitoxantrone---anti neoplastic
    ( An eighth, cladribine is currently awaiting an FDA decision on its approval)
  13. samuel

    samuel New Member

    RITUXIMAB---chimeric monoclonal antibody that targets CD20 B lymphocytes

    ---approved for the treatment of active rheumatoid arthritis when combined with methotrexate
    ---useful in CLL/SLL and NHL
  14. samuel

    samuel New Member


    oral bioavailability - excellent (~ 90%) not food-dependent
    highly lipophilic (CSF conc 45% of plasma)
    extensively metabolised by CYP primarily thro urine(moderate inducer of CYP3A)

    rash(typically within 4 to 6 wks) app 17%(but dose limiting in 7% only)
    hepatotoxic 4%(more freq with women,pre therapy CD4 count high,co existent hep B or C)
    rarely fulminant

    prevents mother to child transmission
    resistance has emerged
  15. samuel

    samuel New Member

    drugs that increase ICP

  16. samuel

    samuel New Member

    Trimetazidine is an anti-ischemic (anti-anginal) metabolic agent, which improves
    myocardial glucose utilization through inhibition of
    fatty acid metabolism, also known as fatty acid oxidation inhibitor.
    Medical uses
    Trimetazidine usually prescribed as a long-term treatment of angina pectoris, and in some countries (including France) for tinnitus and dizziness. It is taken twice a day. In 2012 European Medicines Agency (EMA) finished a review of benefits and risks of trimetazidine and recommended restricting use of trimetazidine-containing medicines just as an additional treatment of angina pectoris in case of inadequate control by or intolerance to first-line antianginal therapies.
  17. samuel

    samuel New Member

    TYPE 1 DM--
    :OTELIZUMAB-anti cd 3 antibody,decreases the load of slf reacting lymphocytes
    :DIA PEP 277--similar mech
    :TOL 3021--similar

    TYPE 2 DM--
    :ALEGLITAZAR-double PPARgamma agonist
    :EXANATIDE--GLP 1 analog..decrease glucagoan,increse insulin secretion,promotes staiety..and hence cause wt loss
    :DPP-4 INHIBITORS--prevent endogenous glp1 brakdown,increase action of glp hence(sitagliptan vildagliptan...)

    colsevalam.-bile acid sequestant

    bromocriptine recntly approved too(bihar 2013 question)

    GLIFLOZIN--- Inhibit renal SGLT2 so increase glyccosuria,consequently increas UTI(bihar 2013)

    IMEGLUMIN--oxidative phosphorylation to decrease b.g.

    PRAMILINTIDE--amylin analog,decreases glucagoan,

    decreases cataract in dm--EPALRESTAT!!(INHIBIT Sorbitol metabolism)
  18. samuel

    samuel New Member



    ANAKINRA --IL1 #


    ANTI CD 20--ofatuzumab,ocrelizumab


  19. samuel

    samuel New Member

    Midodrine is a prodrug that is enzymatically hydrolyzed to desglymidodrine, an 1-receptor-selective agonist.
    The peak concentration of desglymidodrine is achieved about 1 hour after midodrine is administered.
    The primary indication for midodrine is the treatment of postural hypotension, typically due to impaired autonomic nervous system function.

    Although the drug has efficacy in diminishing the fall of blood pressure when the patient is standing, it may cause hypertension when the subject is supine.
  20. samuel

    samuel New Member

    terfenadine---metabolised to carboxy metabolite

    metabolite----pharm action
    terfenadine itself----adverse effect---polymorphic vent tachycardia

    metab by CYP3A4
  21. samuel

    samuel New Member

    Other specific types of diabetes
    Genetic defects of beta cell function characterized by mutations in:
    1. Hepatocyte nuclear transcription factor (HNF) 4 ---(MODY 1)
    2. Glucokinase--- (MODY 2)
    3. HNF-1 ---(MODY 3)
    4. Insulin promoter factor-1 ---(IPF-1; MODY 4)
    5. HNF-1 ---(MODY 5)
    6. NeuroD1 ---(MODY 6)
  22. samuel

    samuel New Member

    Glucagon has a potent inotropic and chronotropic effect on the heart, mediated by the cAMP mechanism described above. Thus, it produces an effect very similar to that of -adrenoceptor agonists without requiring functioning receptors
  23. samuel

    samuel New Member

    Z drugs

    zolpidem---decreases REM minimal effect on NREM
    omega 1 subtype selectivity
    little effect on sleep architecture
    less rebound insomnia
    Zaleplon---decreased latency of sleep onset
    no effect on sleep total time,NREM,REM
    eszopiclone---Increased total sleep time
    higher doses decreases REM sleep

    (more rapid onset of sleep and stage 2 NREM prolongation are clinically useful effects)
  24. samuel

    samuel New Member


    therapeutic conc----0.5 to 1.4 ng/mL
    toxic conc----->2.5 ng/mL

    not extensively metabolised--2/3 excreted unchanged
    (clearance proportionate to creatinine clearance)

    inhibit na k ATPase
  25. samuel

    samuel New Member

    aviptidil---VIP analogue useful in erectile dysfunction

    Icatibant ----- second-generation B2 receptor antagonist
    orally active, potent, and selective
    has a long duration of action (> 60 minutes)
    displays high B2-receptor affinity in humans

    (B-----bradykinin receptor not beta receptor)
  26. samuel

    samuel New Member

    geftinib erlotinib=
    tyrosine kinase inhibitors asso with EGFR
    indi_non small lung cancer
    food increases 100% absorbtion
    side effect......acneform skin rash,diarrhea
    metabolised by CYP3A4

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