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| Primary information |
|---|
| ID | 10476 |
| Therapeutic ID | Th1087 |
| Protein Name | Oxytocin |
| Sequence | >Th1087_Oxytocin
CYIQNCPLG
|
| Molecular Weight | 1007.187 |
| Chemical Formula | C43H66N12O12S2 |
| Isoelectric Point | 5.51 |
| Hydrophobicity | -2.7 |
| Melting point | 192-194 ℃ |
| Half-life | 1-6 min |
| Description | 9-residue cyclic peptide, synthetically prepared to avert possible contamination with vasopressin and small polypeptides |
| Indication/Disease | To assist in labor, elective labor induction, uterine contraction induction |
| Pharmacodynamics | Used to induce labor or to enhance uterine contractions during labor. Uterine motility depends on the formation of the contractile protein actomyosin under the influence of the Ca2+-dependent phosphorylating enzyme myosin light-chain kinase. Oxytocin promotes contractions by increasing the intracellular Ca2+, which in turn activates myosins light chain kinase.. Oxytocin has specific receptors in the muscle llining of the uterus and the receptor concentration increases greatly during pregnancy, reaching a maximum in early labor at term. |
| Mechanism of Action | Binds the oxytocin receptor which leads to an increase in intracellular calcium levels. The oxytocin-oxytocin receptor system plays an important role as an inducer of uterine contractions during parturition and of milk ejection. |
| Toxicity | Administration of supratherapeutic doses of exogenous oxytocin can lead to myocardial ischemia, tachycardia, and arrhythmias. High doses can also lead to uterine spasms, hypertonicity, or rupture. Oxytocin has antidiuretic properties, thus, high daily doses (as a single dose or administered slowly over 24 hours) may lead to extreme water intoxication resulting in maternal seizures, coma, and even death. The risk of antidiuresis and water intoxication in the mother appears to be greater when fluids are given orally |
| Metabolism | Oxytocin is rapidly removed from the plasma by the liver and kidney. The enzyme oxytocinase is largely responsible for the metabolism and regulation of oxytocin levels in pregnancy and only a small percentage of the neurohormone is excreted in the urine unchanged.Oxytocinase activity increases throughout pregnancy and peaks in the plasma, placenta and uterus near term. The placenta is a key source of oxytocinase during gestation and produces increasing amounts of the enzyme in response to increasing levels of oxytocin produced by the mother. Oxytocinase activity is also expressed in mammary glands, heart, kidney, and the small intestine.Lower levels of activity can be found in the brain, spleen, liver, skeletal muscle, testes, and colon. The level of oxytocin degradation is negligible in non-pregnant women, men, and cord blood |
| Absorption | Oxytocin is administered parenterally and is fully bioavailable. It takes approximately 40 minutes for oxytocin to reach steady-state concentrations in the plasma after parenteral administration. |
| NA |
| Clearance | In a study that observed 10 women who were given oxytocin to induce labor, the mean metabolic clearance rate was 7.87 mL/min. |
| Categories | Oxytocics, Anti-tocolytic Agents and Labor Induction Agents |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Oxytocin receptor |
| Brand Name | Pitocin |
| Company | JHP Pharmaceuticals |
| Brand Description | JHP Pharmaceuticals |
| Prescribed For | Induction or Stimulation of Labor, Control of Postpartum Uterine Bleeding, Treatment of Incomplete, Inevitable, or Elective Abortion |
| Chemical Name | NA |
| Formulation | NA |
| Physical Appearance | Pitocin (oxytocin injection, USP) is a sterile, clear, colorless aqueous solution of synthetic oxytocin, for Intravenous infusion or intramuscular injection. Pitocin is a nonapeptide found in pituitary extracts from mammals. It is standardized to contain 10 units of oxytocic hormone/mL and contains |
| Route of Administration | Intravenous infusion |
| Recommended Dosage | initial dose should be 0.5–1 mU/min (equal to 3–6 mL of the dilute oxytocin solution per hour). At 30–60 minute intervals the dose should be gradually increased in increments of 1–2 mU/min until the desired contraction pattern has been established. |
| Contraindication | Do NOT use Pitocin if: you are allergic to any ingredient in Pitocin; your birth canal is too small compared with the fetus's head; you have other complications that require medical intervention for birth; you have bacteria in the blood; you cannot have a child through vaginal delivery because of certain conditions (eg, genital herpes, cervical cancer) |
| Side Effects | Symptoms of overdose: Restlessness, shakiness, sleepiness, slow to respond, slurred speech, unconsciousness. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |