Ergot Observatives

Ergot Observatives 

These two are extensively used as oxytocics:

• Ergometrine

• Methergine

Ergotamine:

It is an alkaloid isolated by Dualey and Moir in 1935 from Ergot, a fungus Claviceps Purpura, that is used as oxytocics agent. It produce uterine contraction in the upper as well as lower segment and used to control PPH.

Mechanism of Action

• Ergotamine
  • It has partial agonist action on 5 HT2 and alpha adrenergic receptor.
  • Causes contraction of uterus.

Causes Contraction of Uterus

• At low dose contraction are phasic with normal relaxation in between, but only moderate increase in dose raises the basal tone and contraction occur in high doses.
• Graid uterus is more sensitive at term and in Early Puerperium.

Indication

• Post portum Haemorrhage.
• Migraine.
• Vascular Headache.
• Post abortion.
• Menopausal Hot Flashes.

ADR

• Abnormal Heart valve finding (Chronic use).
• Arrhythmia.
• Tachy Cardia.
• Numbness of Extremities.
• Abdominal pain.
• Possible gangrene.
• Pruritis.
• Vomiting.
• Angina.
• Vasoconstriction.
• Fatigue.
• Rebound Headache.
• Ergotism.
• Parasthesia.
• Nausea.
• Muscle weakness.

Contraindication

• Hypersensitivity.
• CAD.
• PVD.
• Pregnancy/location.
• Impaired renal or Hepatic function.
• Severe HTN.
• Sepsis.
• Malnutrition.
• Toxemia Pregnancy.
• Case of threatened spontaneous Abortion.
• Concomitant Strong CYP3A4 inhibitors.
• Prolonged use.

Caution

• Should begin as soon as a vascular headache initially appears.
• Headache ineffective for muscular contraction.
• Stop if circulation is impeded in S/S.
• Paresthesia, Gl disturbance, and chest pain are all possible.
• May make heart failure worse.
• Safety not proven for children.
• It shouldn't be used during pregnancy, the first or second stage of labor, or just before the head is crowned.

Dosage forms (Pregnancy category)

• Ampoules (0.25-0.5 mg).
• Tablet (0.5-1 mg).

Dose:

• 0.5 mg IM, may repeat in 2-4 hrs, not exceed 5 dose total.
• Give IV in Emergency.
• Alternatively, 0.2-0.4 mgxpo 6-12 hrs PRN for 48 hrs, not more than 1 weeks.

Pharmacokinetics:

• Half-life: Elimination 1.5-2 hr.
• Metabolism: Liver by CRP3A4.
• Excretion: 90% bile.
• Distribution: Cross BBB and Enter Breast milk.
• Absorption: 60% from GI tract.

Nursing Consideration:

• Tell the patient to take ergotamine as soon as a headache threatens, but not to take more than the recommended amount.
• After taking the medicine, encourage the patient to relax in a dark, quiet space.
• Review the poisonous symptom. Tell the patient to report them right away.
• Reminding the patient not to smoke and not to expose themselves to the cold Vasoconstrictor medications may make peripheral circulation even worse.
• May make you feel queasy. Before the drug's reaction is known, advise the patient to refrain from driving and engaging in other tasks that call for attentiveness.
• Tell the patient to stay away from alcohol because it can cause vascular headaches. Fit Instruct the female patient to let the doctor know if she intends to become pregnant or suspects it.