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    1-Drugs Affecting Uterine Muscle Contractility

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    jojolilimomo
    1. The document discusses drugs that affect uterine muscle contractility, including oxytocin, ergot alkaloids, and prostaglandins which produce contractions, and beta-adrenoceptor agonists, calcium channel blockers, and prostaglandin synthetase inhibitors which produce relaxation. 2. Oxytocin causes physiological contractions of the uterus, especially the fundus, while ergot alkaloids cause tetanic contractions. Prostaglandins contract the uterus throughout pregnancy and soften the cervix. 3. Tocolytic drugs that cause uterine relaxation include beta-adrenoceptor agonists like ritodrine, calcium channel blockers like nifedipine, and NSA

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    1-Drugs Affecting Uterine Muscle Contractility

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    jojolilimomo
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    1. The document discusses drugs that affect uterine muscle contractility, including oxytocin, ergot alkaloids, and prostaglandins which produce contractions, and beta-adrenoceptor agonists, calcium channel blockers, and prostaglandin synthetase inhibitors which produce relaxation. 2. Oxytocin causes physiological contractions of the uterus, especially the fundus, while ergot alkaloids cause tetanic contractions. Prostaglandins contract the uterus throughout pregnancy and soften the cervix. 3. Tocolytic drugs that cause uterine relaxation include beta-adrenoceptor agonists like ritodrine, calcium channel blockers like nifedipine, and NSA

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    1. The document discusses drugs that affect uterine muscle contractility, including oxytocin, ergot alkaloids, and prostaglandins which produce contractions, and beta-adrenoceptor agonists, calcium channel blockers, and prostaglandin synthetase inhibitors which produce relaxation. 2. Oxytocin causes physiological contractions of the uterus, especially the fundus, while ergot alkaloids cause tetanic contractions. Prostaglandins contract the uterus throughout pregnancy and soften the cervix. 3. Tocolytic drugs that cause uterine relaxation include beta-adrenoceptor agonists like ritodrine, calcium channel blockers like nifedipine, and NSA

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    79 views40 pages

    1-Drugs Affecting Uterine Muscle Contractility

    Uploaded by

    jojolilimomo
    1. The document discusses drugs that affect uterine muscle contractility, including oxytocin, ergot alkaloids, and prostaglandins which produce contractions, and beta-adrenoceptor agonists, calcium channel blockers, and prostaglandin synthetase inhibitors which produce relaxation. 2. Oxytocin causes physiological contractions of the uterus, especially the fundus, while ergot alkaloids cause tetanic contractions. Prostaglandins contract the uterus throughout pregnancy and soften the cervix. 3. Tocolytic drugs that cause uterine relaxation include beta-adrenoceptor agonists like ritodrine, calcium channel blockers like nifedipine, and NSA

    Copyright:

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    Download as PPT, PDF, TXT or read online from Scribd
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    1-DRUGS AFFECTING UTERINE MUSCLE CONTRACTILITY

    DRUGS PRODUCING UTERINE CONTRACTIONS( Oxytocic Drugs )

    Oxytocin Syntocinon

    Ergot Alkaloids Ergometrine (Ergonometrine)

    Prostaglandins PGE2 PGF2

    OXYTOCIN (Syntocinon )
    R

    Synthesis

    It is a posterior pituitary hormone secreted by the posterior pituitary gland, which is originally synthesized by the hypothalamus.
    Oxytocin secretion occurs by sensory stimulation from areas of the cervix ,vagina , and by suckling at the breast.

    Oxytocin causes contraction of the fundus only.

    Pharmacokinetics of oxytocin
    Absorption, Metabolism and Excretion

    Not effective orally Administered intravenously* Also as nasal spray (to improve milk ejection, 2-3 minutes before breast feeding) Not bound to plasma proteins Catabolized by liver & kidneys Half life = 5 minutes
    *S.C or IM difficult to monitor

    Role of oxytocin

    Uterus

    Stimulates both the frequency and force of uterine contractility particularly of the fundus segment of the uterus.
    These contractions resemble the normal physiological contractions of uterus (contractions followed by relaxation)

    Immature uterus is resistant to oxytocin.

    Causes the contraction of at-term uterine smooth muscles only. Sensitivity increases to 8 fold in the last 9 weeks and 30 times in early labor. Clinically oxytocin is given only when uterine cervix is soft and dilated. see next slide

    oxytocin is not given to induce abortion because the cervix is not dilated (too early)

    before labor the cervix is closed Oxytocin isnt used at this stage

    At term the cervix is fully dilated Oxytocin is used at this stage

    Mechanism of action
    Intracellular fluid Extracellular fluid Oxytocin stimulates Ca++ to interact with its receptor Oxytocin

    Myometrial cell

    Contraction occurs Ca++ Receptor

    N.B. Oxytocin also causes the release of Ca++ from the sacroplasmic reticulum

    Therapeutic Uses of Oxytocin


    1. Induction & augmentation of labor (remember only slow IV infusion)

    Mild preeclampsia (a serious condition developing in late pregnancy, characterized by sudden hypertension, proteinuria, and edema) Uterine inertia (Uterine atony) Incomplete abortion Post maturity (post-term fetus) Maternal diabetes

    Therapeutic Uses of Oxytocin (continue)

    2. Postpartum uterine hemorrhage (IV drip) (ergometrine is often used nowadays)


    3. Impaired milk ejection
    One puff in each nostril 2-3 min before nursing

    Side effect

    Maternal death due to

    Water intoxication B/C it is a weak antidiuretic

    Fetal death due to

    Uterine rupture (occurs at high doses)

    Hypertension

    Constiction of placental blood vessels Ischemia

    Hypersensitivity to oxytocin

    Cephalopelvic disproportion

    Prematurity
    Contraindications

    Abnormal fetal position horizontal

    Evidence of fetal distress

    Cephalopelvic disproportion
    Fetuss head is much larger than the pelvic outlet.

    Multiple pregnancy

    precaution
    Previous cesarean section*

    Hypertension

    *to avoid rupture of the uterus

    Ergot alkaloids
    Ergometrine (Ergonovine)

    Methylergonovine (synthetic)

    Effects on the Uterus

    Alkaloid derivatives induce TETANIC CONTRACTION of uterus without relaxation in between (unlike the normal physiologic contractions)

    It causes contractions of the uterus as a whole i.e. fundus and cervix (tends to compress rather than actually expelling the fetus) Not used anymore for labor augmentation.

    Sites of ergot contraction

    Ergot alkaloids (pharmacokinetics)

    Absorption fate and excretion

    Absorbed orally from the GIT (tablets) Usually given IM NOT given IV because it causes severe vasoconstriction Extensively metabolized in the liver 90% of metabolites are excreted in bile Uterus responds to Ergots more than Oxytocin

    Clinical uses

    Postpartum hemorrhage (used only at the 3rd stage of labor, when the babys head or shoulder start to appear)

    Preparations
    ergometrine 0.5 mg

    Syntometrine I.M
    oxytocin 5.0

    If used I.V blood pressure

    Why should we use this combination ? Ergots have slow onset of action (7min) but have a long half-life. Yet, oxytocin has a fast onset of action, 1-2 minutes, with a short half-life.

    Side effects
    Nausea, vomiting, diarrhea Hypertension because contraction of blood vessels Vasoconstriction of peripheral blood vessels ( toes & fingers) which can lead Gangrene


    1.

    Contraindications:

    Induction of labour 2. 1st and 2nd stage of labor 3. vascular disease 4. Severe hepatic and renal impairment 5. Severe hypertension

    PROSTAGLANDINS (PGE2 & PGF2) Therapeutic uses


    1. Induction of abortion (pathological)** (used because the uterus is sensitive to PGs in early stages). 2. Induction of labor (fetal death in utero) 3. Postpartum hemorrhage

    Difference between PGS and Oxytocin:

    PGs contract uterine smooth muscle not only at term(as with oxytocin), but throughout pregnancy.

    PGs soften the cervix; whereas oxytocin does not.


    PGs have longer duration of action than oxytocin.
    N.B. PGs at low doses physiologic contraction at high doses Tetanic contraction

    Side Effects
    Nausea , vomiting Abdominal pain Diarrhea Bronchospasm (PGF2) Flushing (PGE2). P.S. PGE2 causes vasodilation of the mothers vessels thus leading to cutaneous flushing. Yet, there is vasoconstriction of the umbilical cords vessels. PGE2 is used as a vaginal suppository for cervical dilation and softening.

    Contraindications: Mechanical obstruction of delivery Fetal distress (due to umbilical cord vessels vasocontriction) Predisposition to uterine rupture
    Precautions: Asthma Multiple pregnancy Glaucoma Uterine rupture

    Difference B/W Oxytocin and Prostaglandins


    Character Contraction Oxytocin Only at term Prostaglandins Contraction through out pregnancy

    Cervix

    Does not soften the cervix

    soften the cervix

    Contd
    Character Duration of action Oxytocin Shorter Prostaglandins Longer

    uses

    Induce and augment labour and post partum hemorrhage

    Induce abortion in 2nd trimester of pregnancy. Used as vaginal suppository (PGE2) for induction of labor

    Difference b/w Oxytocin and Ergometrine


    Character Oxytocin Ergometrine Tetanic contraction ; doesn't resemble normal physiological contractions Only in postpartum hemorrhage

    Contractions Resembles normal physiological contractions Uses To induce &augment labor. *Post partum hemorrhage Rapid onset Shorter duration of action

    Onset and Duration

    Moderate onset Long duration of action

    2-UTERINE RELAXANTS

    DRUGS PRODUCING UTERINE RELAXATION (Tocolytic Drugs) Action and Uses Relax the uterus and arrest threatened abortion or delay premature labor.
    1.-ADRENOCEPTOR AGONISTS** Ritodrine, i.v. drip Selective 2 receptor agonist used specifically as a uterine relaxant.
    Tocolytic drugs: drugs that cause inhibition of premature labor.

    - adrenoceptor agonists e.g. 2 selective agonists: ritodrine

    Mechanism of action
    Bind to -adrenoceptors activating the enzyme adenylate cyclase increasing the level of cAMP reducing intracellular calcium level.

    As the pregnancy progresses there is gradual increase of uterine 2 receptors. This is an attempt to increase 2 responsiveness to its agonist, an
    important role for the stability of fetal growth.

    Side effects: Tremor Nausea , vomiting Flushing Sweating Tachycardia (high dose) Hypotension Hyperglycemia Hypokalaemia

    2.CALCIUM CHANNEL BLOCKERS Nifedipine


    Causes relaxation of the myometrium Markedly inhibits the amplitude of spontaneous and oxytocin-induced contractions.

    Unwanted effects

    Headache, dizziness Hypotension Flushing Constipation Ankle edema Coughing Wheezing Reflex tachycardia

    3. Prostaglandin synthetase inhibitors

    The depletion of prostaglandins prevents stimulation of uterus

    NSAID,s e.g. Indomethacin Aspirin Ibuprofen

    Adverse effects Ulceration Premature closure of ductus arterious.

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