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    Oxytocics: Prepared By: Mirza Anwar Baig

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    revathidadam55555
    Oxytocics are drugs that stimulate uterine contractions. This document discusses oxytocic drugs including oxytocin, ergot alkaloids like ergometrine, and prostaglandins like PGE2 and PGF2α. It provides details on their mechanisms of action, pharmacokinetics, therapeutic uses, and differences between the classes of drugs. The key information is their use for labor induction, augmentation and postpartum hemorrhage as well as their varying effects on uterine contractions and cervical softening.

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    Oxytocics: Prepared By: Mirza Anwar Baig

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    revathidadam55555
    281 views28 pages
    Oxytocics are drugs that stimulate uterine contractions. This document discusses oxytocic drugs including oxytocin, ergot alkaloids like ergometrine, and prostaglandins like PGE2 and PGF2α. It provides details on their mechanisms of action, pharmacokinetics, therapeutic uses, and differences between the classes of drugs. The key information is their use for labor induction, augmentation and postpartum hemorrhage as well as their varying effects on uterine contractions and cervical softening.

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    Oxytocics are drugs that stimulate uterine contractions. This document discusses oxytocic drugs including oxytocin, ergot alkaloids like ergometrine, and prostaglandins like PGE2 and PGF2α. It provides details on their mechanisms of action, pharmacokinetics, therapeutic uses, and differences between the classes of drugs. The key information is their use for labor induction, augmentation and postpartum hemorrhage as well as their varying effects on uterine contractions and cervical softening.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    281 views28 pages

    Oxytocics: Prepared By: Mirza Anwar Baig

    Uploaded by

    revathidadam55555
    Oxytocics are drugs that stimulate uterine contractions. This document discusses oxytocic drugs including oxytocin, ergot alkaloids like ergometrine, and prostaglandins like PGE2 and PGF2α. It provides details on their mechanisms of action, pharmacokinetics, therapeutic uses, and differences between the classes of drugs. The key information is their use for labor induction, augmentation and postpartum hemorrhage as well as their varying effects on uterine contractions and cervical softening.

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    © All Rights Reserved
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    of 28

    OXYTOCICS

    Prepared by: Mirza Anwar Baig


    M.Pharm (Pharmacology)
    Anjuman I Islam's Kalsekar Technical Campus,
    School of Pharmacy.
    New Panvel,Navi Mumbai

    Compiled by: Prof. Anwar Baig 1


    OXYTOCICS
    • Oxytocics are the drugs of varying
    chemical nature that have the power to
    stimulate the contraction of uterine
    muscles.
    • Also called Uterotonics
    • The introduction of oxytocic drugs for
    the treatment of Post Partum
    Hemorrhage (PPH) has been regarded as
    “ one of the enduring achievements of
    modern science”.

    Compiled by: Prof. Anwar Baig 2


    DRUGS PRODUCING UTERINE
    CONTRACTIONS( Oxytocic Drugs )
    1. OXYTOCIN
    2. ERGOT ALKALOIDS
    Ergometrine (Ergonovine)
    3. PROSTAGLANDINS
    a) PGE2
    b) PGF2α

    4. MISCELLANEOUS
    Quinine
    Emetine
    Alcohol
    Ethacridine

    Compiled by: Prof. Anwar Baig 3


    1.Oxytocin

    i.Synthesis of Oxytocin:

    • Is a posterior pituitary hormone


    secreted by the posterior pituitary
    gland.

    • Oxytocin secretion occurs by sensory


    stimulation from cervix ,vagina , and
    from suckling at breast.

    Compiled by: Prof. Anwar Baig 4


    ii. Secretion of oxytocin:

    Compiled by: Prof. Anwar Baig 5


    iii. Pharmacodynamics

    UTERUS
    •Oxytocin acts through G protein-coupled receptors and the
    phosphoinositide -calcium second-messenger system to
    contract uterine smooth muscle.

    •Oxytocin also stimulates the release of prostaglandins and


    leukotrienes that augment uterine contraction.

    •Oxytocin in small doses increases both the frequency and


    the force of uterine contractions.

    •At higher doses, it produces sustained contraction.

    Compiled by: Prof. Anwar Baig 6


    i
    •These contractions resemble the normal
    physiological contractions of uterus
    (contractions followed by relaxation)

    •Immature uterus is resistant to oxytocin.

    •Contract uterine smooth muscle only at


    term.

    • Sensitivity increases to 8 fold in last 9


    weeks and 30 times in early labor.

    Compiled by: Prof. Anwar Baig 7


    Mechanism of action

    The interaction of endogenous or administered


    oxytocin , with myometrial cell membrane receptor
    promotes the influx of ca++ from extra cellular
    fluid and from S.R in to the cell , this increase in
    cytoplasmic calcium ,stimulates uterine contraction .

    Compiled by: Prof. Anwar Baig 8


    Compiled by: Prof. Anwar Baig 9
    BREAST
    • Oxytocin also causes contraction of
    myoepithelial cells surrounding mammary
    alveoli, which leads to milk ejection.
    • Used in breast engorgement

    KIDNEYS
    • At high concentrations, oxytocin has weak
    antidiuretic and pressor activity due to
    activation of vasopressin receptors.

    Compiled by: Prof. Anwar Baig 10


    iv.Pharmacokinetics of oxytocin
    Absorption ,Metabolism and Excretion

    • Not effective orally


    • Administered intravenously
    • Also as nasal spray
    • Not bound to plasma proteins
    • Catabolized by liver & kidneys
    • Half life = 5 minutes
    • Duration of action-20min
    • Stored at 2-8 0C

    Compiled by: Prof. Anwar Baig 11


    v. Therapeutic Uses of Oxytocin

    1. Induction & augmentation of labor (slow I.V infusion)


    Uterine inertia
    Incomplete abortion
    Post maturity

    2. Post partum uterine hemorrhage (I.V drip)

    3. Impaired milk ejection


    One puff in each nostril 2-3 min before nursing

    Compiled by: Prof. Anwar Baig 12


    vi.Side Effects:

    a) Hypertension
    b) Uterine rupture
    c) Fetal death(ischaemia)
    d) Water intoxication
    e) Neonatal jaundice

    Compiled by: Prof. Anwar Baig 13


    2.Ergot Alkaloids
    • Ergot is the natural alkaloid of Claviceps purpurea that
    grows on rye, wheat and other grains.
    • Ergometrine (Ergonovine)
    • Methylergonovine
    i. Chemistry
    • The ergot alkaloids are derivatives of the tetracyclic
    compound 6-methylergoline.
    • The first pure ergot alkaloid ergotamine was obtained
    in 1920, followed by the isolation of
    ergometrine/ergonovine in 1932.
    • The therapeutically useful natural alkaloids are amide
    derivatives of d-lysergic acid.
    • Semi-synthetic derivatives are obtained from catalytic
    hydrogenation of the natural alkaloids.
    e.g.- Methergin (methylergonovine)
    Compiled by: Prof. Anwar Baig 14
    ii. Pharmacodynamics:

    a. Effects on the Uterus

    •Alkaloid derivatives induce TETANIC CONTRACTION


    of uterus without relaxation in between. These does
    not resemble the normal physiological contractions

    • It causes contractions of uterus as a whole i.e.


    fundus and cervix (tend to compress rather than to
    expel the fetus)

    (Difference between oxytocin & ergots)

    Compiled by: Prof. Anwar Baig 15


    b. Vascular effects:
    Direct peripheral vasoconstriction
    In large doses causes damage to capillary
    endothelium.
    Example: Ergotamine and DHE
    c. Gastrointestinal effect:
    Increased in peristaltic activity.
    d. Miscellaneous effect:
    5HT partial agonist
    5HT selective antagonist

    Compiled by: Prof. Anwar Baig 16


    iii.Pharmacokinetics

    • Absorbed orally from GIT(tablets)

    • Usually given I.M

    • Extensively metabolized in liver.

    • 90% of metabolites are excreted in bile

    Compiled by: Prof. Anwar Baig 17


    iv. THERAPEUTIC USES:
    1.POSTPARTUM HEMORRHAGE:-
    • The uterus at term is extremely sensitive to the stimulant
    action of ergot and even moderate doses produce a
    prolonged and powerful spasm of the muscle quite unlike
    natural labor.

    • Therefore, ergot derivatives should be used only for control


    of late uterine bleeding and should never be given before
    delivery.

    • Oxytocin is the preferred agent for control of postpartum


    hemorrhage but if this is ineffective,ERGOMETRINE (0.2
    mg ) is given intramuscularly.

    • It is usually effective within 1–5 minutes and is less toxic


    than other ergot derivatives for this application.
    Compiled by: Prof. Anwar Baig 18
    v.Side effects:
    a) Nausea, vomiting, diarrhea
    b) Hypertension
    c) Vasoconstriction of peripheral blood Vessels (toes &
    fingers)
    d) Gangrene

    Compiled by: Prof. Anwar Baig 19


    vi. Contraindications:
    a) 1st and 2nd stage of labor
    b) vascular disease
    c) impaired hepatic and renal functions

    vii.Precautions:
    a) Cardiac diseases
    b) Hypertension
    c) Multiple pregnancy

    Compiled by: Prof. Anwar Baig 20


    Difference b/w Oxytocin and Ergometrine
    Character Ergometrine Oxytocin
    Contractions Tetanic contraction; Resembles normal
    doesn't resemble physiological
    normal physiological contractions
    contractions

    Uses Only in P.partum *To induce &


    hemorrhage augment labor.
    *Post partum
    hemorrhage
    Onset and Moderate onset Rapid onset
    Duration Long duration of Shorter duration of
    action action

    Compiled by: Prof. Anwar Baig 21


    3.PROSTAGLANDINS (PGE2 & PGF2α)

    i. MECHANISM OF ACTION:
    • Contract uterine smooth muscle

    Difference between PGS and Oxytocin:

    1. PGS contract uterine smooth muscle not only at


    term(as with oxytocin), but throughout pregnancy.

    2. PGS soften the cervix; whereas oxytocin does not.

    3. PGS have longer duration of action than oxytocin.


    Compiled by: Prof. Anwar Baig 22
    PG analogues & Common Preprations
    PGE1 (methyl ester) – MISOPROSTOL
    PGE2 – DINOPROSTONE
    (NOTE: less toxic, more effective so widely used.)
    PGF 2ά- DINOPROSTONE TROMETHAMINE
    PGF2ά (methyl analogue) – CARBOPROST

    Preparations:
    Tablet: 0.5mg dinoprostone (prostinE2)
    Vaginal suppository: 20mg PGE2 /50mg PGF2ά lipid base
    Vaginal pessary: 3mg PGE2
    ProstinE2 gel: 500μg into cervical canal, below internal OS/1-
    2mg in the posterior fornix.
    Parenteral:-
    PGE2 - ProstineE2 1mg/ml
    PGF2ά-ProstinF2 ά(Dinoprost tromethamine) 5mg/ml
    Compiled by: Prof. Anwar Baig 23
    Methyl analogue of PGF2ά- Carboprost 2.5mg/10ml vial
    ii. Therapeutic uses
    1. Induction of abortion (pathological)**

    2. Induction of labor (fetal death in utero)

    3. Postpartum hemorrhage

    Compiled by: Prof. Anwar Baig 24


    iii. Side Effects

    a) Nausea , vomiting
    b) Abdominal pain
    c) Diarrhea
    d) Bronchospasm (PGF2α)
    e) Flushing (PGE2)

    Compiled by: Prof. Anwar Baig 25


    iv. Contraindications:
    a) Mechanical obstruction of
    delivery
    b) Fetal distress
    c) Predisposition to uterine
    rupture

    v. Precautions:
    a) Asthma
    b) Multiple pregnancy
    c) Glaucoma
    d) Uterine rupture
    Compiled by: Prof. Anwar Baig 26
    Difference B/w Oxytocin and Prostaglandins

    Character Prostaglandins Oxytocin

    Contraction Contraction through Only at term


    out pregnancy

    Cervix Soften the cervix Does not soften the


    cervix
    Duration of Longer Shorter
    action
    uses i. Used for abortion i.Not used for
    in 2nd trimester of abortion
    pregnancy. ii.Used for induction
    ii.Used as vaginal and augmentation of
    suppository for labor and post
    induction
    Compiledof labor
    by: Prof. Anwar Baig partum27 hemorrhage
    THANK YOU

    Compiled by: Prof. Anwar Baig

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