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OXYTOCIC / UTEROTONIC
Stimulation
UTERUS CONTRACTION
* Oxytocin
* Derivat Ergot alkaloids
* Derivat Prostaglandin
Oxytocin
(Posterior pituitary hormone)
Pharmacokinetic :
* Route of administration : i.v & buccal absorption
Also as nasal spray (impaired milk ejection)
* Swallowed inactive
* Not bound to plasma protein
* Catabolized by the kidneys & liver
* Circulating t 1/2 : 5 minutes
Mechanism of action :
Interaction myometrial cell membrane receptor promotes the influx of Ca++ from extra cellular
fluid and from S.R in to the cell
cytoplasmic calcium
Pharmacodynamic :
Alters transmembrane ionic currents in myometrial smooth muscle cells & myoepithelial cells of
mammary alveoli
Uterus
Stimulates both the frequency and force of uterine contractility particularly of the fundus
segment of the uterus
Clinical application :
* Diagnostic : placental circulatory condition
* Therapeutic :
= Induce labor (slow i.v infusion)
= Augment dysfunctional labor for :
1. Conditions requiring early vaginal delivery:
Rh problem, maternal diabetes,
preeclampsia & post maturity
2. Uterine inertia
3. Incomplete abortion
* Therapeutic
= Post partum uterine hemorrhag (i.v drip)
(ergometrine is often used)
= Impaired milk ejection
One puff in each nostril 2-3 min before nursing
= Preparation available : Syntocinon & pitocin
Adverse reaction :
* Maternal death hypertensive episodes
* Uterine rupture
* Water intoxication
* Fetal death
* Afibrinogenemia
Contra indication :
* Fetal distress
* Prematurity
* Abnormal fetal presentation
* Cephalo-pelvic disproportion
Precautions
Multiple pregnancy
Previous sectio caecarean
Hypertension
Ergot alkaloids
Adrenoceptors
ERGOT ALKALOIDS
Dopamine receptors
5-HT receptors
Histamine
Claviceps purpurea
Acetylcholine
Tyramine
Pharmacokinetics:
Ergotamine:
- oral dose > i.m
- Speed of absorption & peak blood level
improved by caffeine
Amine alkaloids:
- Ergonovine / ergometrine / methylergonovine
- Also absorbed from rectum, buccal cavity, aerosol inhaler
- After i.m : slow absorption but reliable
- Metabolism : liver
F153 binder notes
Pharmacodynamics:
Stimulant effects on the uterus:
Sensitivity:
Ergonovine / methylergonovine:
Alkaloid derivatives induce TETANIC CONTRACTION without relaxation in between (not like
normal physiological contractions)
Clinical application:
or immediately afterward
if bleeding is significant
Side effects : Nausea, vomiting, BP
Toxicity:
g.i.t disturbancies : diarrhea, nausea, vomiting activation of medullary vomiting center
& g.i.t serotonin receptors more dangerous prolonged vasospasm
(toes & fingers gangrene amputation)
Therapy: infusion of large doses
of nitroprusid or nitroglycerin
C.I: vascular disease & collagen disease
Contra indication:
1) Induction of labour:
1st and 2nd stage of labor
2) Vascular disease
3) Severe hepatic & renal impairment
4) Severe hypertension
Oxytocin
Ergometrine
Contractions
Uses
Rapid onset
and Duration
Shorter duration
Moderate onset
of action
Prostaglandin
Uterotonic (PGE2 & PGF2)
Clinical application:
1.
2.
3.
Postpartum hemorrhage
A. Abortion
PGE2 & PGF2 : 1 st & 2 nd trimester abortion proteoglycan & changing biophysical
PGE2 & PGF2 : produced abortion in 80 % of cases rate), i.m, i.v, intravaginal
B. Facilitation of labor
PGE2 & PGF2 have no antidiuretic effect induction labor in woman : preeclampsia,
cardiac & renal disease
Side Effects:
Nausea , vomiting
Abdominal pain, diarrhea
Bronchospasm (PGF2)
Flushing (PGE2)
Contra indications:
Mechanical obstruction of delivery
Fetal distress
Predisposition to uterine rupture
Precautions:
Asthma
Multiple pregnancy
Glaucoma
Uterine rupture
Character
Oxytocin
Prostaglandins
Contraction
Only at term
Contraction through
out pregnancy
Cervix
Character
Oxytocin
Prostaglandins
Duration
action
of
Uses
Shorter
Longer
Induce abortion
2nd trimester
pregnancy
in
of
TOCOLYTIC
Action and Uses
Relax the uterus & arrest threatened abortion or delay premature labor
Clinical application:
Prevention of seizures in eclampsia, not used for arrest of preterm labor for its toxicites
The initial dose is 40 cc of 10% solution given slowly i.v
The subsequent doses: depend upon the response & the development of MgSO4 toxicity so
reflexes and respiratory rate should be observed
Side effects:
-
Respiratory depression
Weakness diplopia
Muscular paralysis
Cardiac arrest
Dosis > 5o mg associated with neonatal brain damage
-adrenoceptor agonists
Tocolytic (-Adrenoceptor agonists)
Ritodrine, i.v. drip
Selective 2 receptor agonist
used specifically as a uterine relaxant
Mechanism of action
Activate enzyme adenylate cyclase the level of cAMP reducing intracellular calcium level
Side effects:
Pulmonary edema
Hyperglycemia
Hypokalaemia
Hypotension, myocardial ischaemia
Tachycardia (high dose), arrythmia
Nausea, vomiting
Flushing, Sweating,
Tremor
Side effects
Transient hipotension
Flushing, constipation
Wheezing, tachycardia
Side effects
Hepatitis
Renal failure
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