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    Antipyretics: Instiaty Tropical Infection Module 2017-2018 Dept of Pharmacology and Therapeutics Fkui

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    salsa2506
    This document discusses common antipyretic drugs, including their mechanisms of action, dosages, and side effects. The main antipyretics discussed are aspirin, ibuprofen, methampyron, and paracetamol. All work by reducing prostaglandin E2 levels in the hypothalamus to lower fever. Aspirin and ibuprofen are NSAIDs that inhibit cyclooxygenase. Methampyron carries risks of agranulocytosis. Paracetamol has weak anti-inflammatory effects and is generally safe, but can cause liver toxicity in high doses.

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    Antipyretics: Instiaty Tropical Infection Module 2017-2018 Dept of Pharmacology and Therapeutics Fkui

    Uploaded by

    salsa2506
    15 views22 pages
    This document discusses common antipyretic drugs, including their mechanisms of action, dosages, and side effects. The main antipyretics discussed are aspirin, ibuprofen, methampyron, and paracetamol. All work by reducing prostaglandin E2 levels in the hypothalamus to lower fever. Aspirin and ibuprofen are NSAIDs that inhibit cyclooxygenase. Methampyron carries risks of agranulocytosis. Paracetamol has weak anti-inflammatory effects and is generally safe, but can cause liver toxicity in high doses.

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    This document discusses common antipyretic drugs, including their mechanisms of action, dosages, and side effects. The main antipyretics discussed are aspirin, ibuprofen, methampyron, and paracetamol. All work by reducing prostaglandin E2 levels in the hypothalamus to lower fever. Aspirin and ibuprofen are NSAIDs that inhibit cyclooxygenase. Methampyron carries risks of agranulocytosis. Paracetamol has weak anti-inflammatory effects and is generally safe, but can cause liver toxicity in high doses.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    15 views22 pages

    Antipyretics: Instiaty Tropical Infection Module 2017-2018 Dept of Pharmacology and Therapeutics Fkui

    Uploaded by

    salsa2506
    This document discusses common antipyretic drugs, including their mechanisms of action, dosages, and side effects. The main antipyretics discussed are aspirin, ibuprofen, methampyron, and paracetamol. All work by reducing prostaglandin E2 levels in the hypothalamus to lower fever. Aspirin and ibuprofen are NSAIDs that inhibit cyclooxygenase. Methampyron carries risks of agranulocytosis. Paracetamol has weak anti-inflammatory effects and is generally safe, but can cause liver toxicity in high doses.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    of 22

    ANTIPYRETICS

    Instiaty
    Tropical Infection Module 2017-2018
    Dept of Pharmacology and Therapeutics
    FKUI
    1
    Antipyretics

    §  Antipyretics are drugs capable of reducing


    body temperatures in patients with fever
    §  Antipyretics do not reduce normal body
    temperature
    §  Mech of antipyretic:
    reducing the level of PGE2 in the
    thermoregulatory center by inhibiting COX
    3
    Mechanism of action of NSAIDs

    NSAIDs

    4
    Commonly used antipyretics
    5

    §  Aspirin
    §  Ibuprofen
    §  Metamizol
    §  Paracetamol


    §  Other NSAIDs such as diclofenac,
    ketoprofen, naproxen, indomethacin :
    ú  produce antipyretic effect in doses
    higher than their analgesic doses
    ú  relatively more toxic compared to classic
    antipyretic

    6
    Aspirin (1)
    q  Acetyl salicylic acid
    q  Mech of act: inhibits biosynthesis of PGE2
    q  Orally: well absorbed → hydrolyzed in the liver
    → salicylic acid → excreted through the kidney
    q  Onset of action is 15-30 min after ingestion and
    lasts for 4-8 hours
    q  Dosage (as antipyretic):
    §  adult: 325 – 650 mg every 4 – 6 h, (max. dose
    3,6 g/day)
    §  children: 10 -15 mg/kg BW every 4 – 6 h,
    Max: 60-80 mg/kg/day
    q  Over-the-counter (OTC) drug
    Aspirin (2)
    8
    q  Side effects:
    §  GI disturbance: abdominal pain, nausea,
    dyspepsia, gastric/duodenal ulcer, diarrhea
    §  Inhibition of platelet aggregation →
    prolonged bleeding time
    §  Reye’s syndrome: may occur (rare) if
    aspirin is given to children with viral
    infection. Symptoms: coma, seizure,
    cerebral edema, acute noninflammatory
    encephalopathy and fatty degenerative
    liver failure, multi-organ failure & death.
    Aspirin (3)
    §  Salicylate intoxication → “salicylism”
    characterized by vomiting, tinnitus, hearing
    loss, hyperventilation, vertigo.
    §  Tinnitus usually occur when plasma level of
    salicylic acid reaches 200-450 µg/mL
    (antipyretic dose of aspirin → plasma level of
    < 60 µg/mL)
    Aspirin (4)

    Contraindications
    §  Active petic ulcer disease.
    §  Haemophilia and other haemorrhagic
    disorders, anticoagulant treatment.
    §  In treatment of viral haemorrhagic fevers
    such as dengue.
    §  Hypersensitive patients, in whom history
    of bronchial asthma, angioedema or
    urticaria have been precipitated by aspirin
    or other NSAIDS.
    10
    Ibuprofen
    q  A propionic acid derivative
    q  Analgesic and antipyretic effect: equal to
    aspirin
    q  Antiinflammatory effect: less than aspirin
    q  Dose:
    q  Adult; 200 mg, 3-4 times daily, max dose

    1200 mg/day
    q  Children: 5-10 mg/kg BW, 3-4 times daily,

    max 40 mg/kg/day for children 2 to 11 years.


    Ibuprofen
    q  Well absorbed following oral administration
    q  onset of action : ± 30 -60 minutes with a
    duration of action of 6 to 8 hours
    q  Side effect: GI disturbances (less than aspirin)
    q  OTC drug
    Methampyron (dipyron, metamizole)
    •  Is a pyrazolon derivative with weak
    antiinflammatory effect
    •  Side effect: agranulocytosis, aplastic
    anemia, thrombocytopenia → prohibited in
    many countries
    •  incidence rate of metamizole-induced
    agranulocytosis is between 0.2 and 2 cases per
    million person days of use, with approximately
    7% of all cases fatal
    Methampyron (dipyron, metamizole)
    •  Indication:
    •  Analgesic and antipyretic for conditions
    failing to respond to the more safe
    agents
    •  When parenteral administration is
    needed
    •  (Note: currently paracetamol IV
    preparation is already available in
    Indonesia)
    Paracetamol (acetaminophen) (1)

    q  Paracetamol has a very weak


    antiinflammatory effect, but it is used in
    arthralgia because of its good analgesic
    effect
    q  Mechanism of antipyretic:
    Inhibition of PGE2 production in the
    preoptic region of hypothalamus
    Paracetamol (2)
    q Pharmacokinetics
    §  Well absorbed through oral route,
    bioavailability 70-90%, metabolized in the
    liver, and excreted through the kidney
    §  Metabolism:
    §  in the liver by conjugation with glucuronic acid
    (55%) and sulfuric acid (35%)
    §  Hepatotoxic and nephrotoxic metabolite N-
    acetyl-p-benzo-quinone imine (NAPQI) are
    produced in small amounts by the cytochrome
    P450 (isoenzyme CYP2E1) àdetoxified by
    conjugation with glutathione (GSH)
    Paracetamol (3)
    q  Pharmacokinetics (cont’d)
    §  T½ is 2-3 hours, but may be doubled if
    very high dose is given
    §  Onset of action: ± 30 min, duration of
    action ± 4 h.
    ú  Max single dose (adult): 1000 mg;
    ú  Max daily dose (adult): 4 g per 24 hours
    ú  Pediatric (2-12 yrs): max single dose 15
    mg/kg, not exeed 750 mg; max daily dose
    75 mg/kg in 24 hors (not exeeding 3750
    mg)
    Paracetamol (4)
    Side effects
    ú  Relatively safe, also in pregnancy
    ú  In therapeutic dose (adult: 3-4 x 500 mg/
    day, children 10-15 mg/kg , 4-6 times daily):
      does not affect the CVS system,
    respiration, platelet function and blood
    coagulation
      Does not irritate or induce bleeding of
    the stomach
    Paracetamol (5)

    Side effects (cont’d)


    ú  In a very high dose (10-15 g or 150-250
    mg/kg BW):
       NAPQI ↑ ↑ → depletion of body GSH
    (glutathion) → liver necrosis. Drug of
    choice for this condition: N-acetylcystein
    (given in 24 h)
    Paracetamol (6)
    §  Use with great caution in patients with
    hepatic dysfunction and in alcoholics.
    §  It is preferable to aspirin in the following
    patient groups:
    ú  Patients with acid peptic disease.
    ú  Patients with bleeding disorders and
    haemophilias.
    ú  Children with viral infections.
    ú  Patients in whom bronchospasm is precipitated
    by aspirin.
    ú  Infants less than 6 months of age..
    ú  Safe in pregnancy and lactation.
    20
    Paracetamol (7)

    §  Preparation:
    §  Oral, rectal, IV
    §  Absorption via the rectal route is highly
    variable and unpredictable – reported
    bioavailability ranging from 24 to 98%
    §  Intravenous paracetamol is only used when
    the oral and rectal routes are not available.

    21
    Thank You

    22

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