Carbetocin (Systemic)


VA CLASSIFICATION
Primary: GU600

Commonly used brand name(s): Duratocin.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).

*Not commercially available in the U.S.



Category:


Oxytocic—

Antihemorrhagic (postpartum uterine bleeding) —

Uterine stimulant—

Indications

Accepted

Atony, uterine (treatment) or
Hemorrhage, postpartum (treatment)—Carbetocin is indicated in the management of uterine atony and postpartum bleeding or hemorrhage following elective cesarean section performed under epidural or spinal anesthesia.{01}

Unaccepted
Appropriate studies have not been performed to establish the safety and efficacy of carbetocin following classical or emergency cesarean section or when anesthesia other than epidural or spinal is used. Safety and efficacy also have not been established following vaginal delivery.{01}


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Source—
     Synthetic analog of oxytocin, a posterior pituitary hormone{01}

Mechanism of action/Effect:

Carbetocin binds to oxytocin receptors present on the smooth musculature of the uterus, resulting in rhythmic contractions of the uterus, increased frequency of existing contractions, and increased uterine tone. The oxytocin receptor content of the uterus is very low in the non-pregnant state, and increases during pregnancy, reaching a peak at the time of delivery.{01}

Onset of action:

Intramuscular — 2 minutes{01}

Intravenous — 2 minutes{01}

Duration of action:

Intravenous — 1 hour {01}

Intravenous — 1 hour{01}


Precautions to Consider

Pregnancy/Reproduction

Pregnancy—
Carbetocin is not indicated during pregnancy, prior to the delivery of the infant{01}. Use of carbetocin during pregnancy could result in hyperstimulation of the uterus with hypertonic or tetanic contractions, tumultuous labor, uterine rupture, cervical and vaginal lacerations, postpartum hemorrhage, uteroplacental hypoperfusion and deceleration of the fetal heart rate, fetal hypoxia, hypercapnea, or death.{01}


Breast-feeding

Carbetocin, in small amounts, has been distributed in the breast milk. This small amount found in breast milk or colostrum after a single injection would not be expected to present a significant safety concern.{01}

There is insufficient evidence to determine whether carbetocin stimulates milk let-down. However, normal let-down occurred in five nursing mothers who received 70 mcg of carbetocin intramuscularly.{01}

Pediatrics

No information is available on the relationship of age to the effects of carbetocin in pediatric patients. Safety and efficacy have not been established.


Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):


Note: There have been no specific drug interactions reported with carbetocin. However, because carbetocin is structurally related to oxytocin, medications that interact with oxytocin may also interact with carbetocin.{01}
Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.

Cyclopropane{01}    (may produce hypotension{01}; maternal sinus bradycardia with abnormal atrioventricular rhythms may also occur{01})


Caudal block anesthesia with a vasoconstrictor{01}    ( may cause severe hypertension{01})


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Except under special circumstances, this medication should not be used when the following medical problem exists:
» Allergy to oxytocin or carbetocin{01}
Risk-benefit should be considered when the following medical problems exist
» Vascular disease, especially coronary artery disease{01}    ( safety and efficacy in the presence of this condition have not been established; if used, extreme caution is recommended{01})




Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence more frequent
    
Abdominal pain {01}
    
flushing {01}(feeling of warmth)
    
headache {01}
    
hypotension {01}(dizziness ; faintness ; or light-headedness)
    
pruritus {01}(itching skin)
    
tremor {01}(trembling)

Incidence less frequent
    
Anemia {01}(pale skin; unusual tiredness or weakness)
    
anxiety {01}(nervousness)
    
chest pain {01}
    
chills {01}
    
dyspnea {01}(shortness of breath)
    
pain {01}
    
tachycardia {01}(fast heartbeat)



Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
    
Nausea {01}
    
vomiting {01}

Incidence less frequent
    
Back pain {01}
    
dizziness {01}
    
metallic taste {01}
    
sweating {01}





Overdose
For more information on the management of overdose or unintentional ingestion, contact a poison control center (see Poison Control Center Listing).

Clinical effects of overdose
The following effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Increased uterine activity {01}

pain {01}

Treatment of overdose
Treatment is generally symptomatic and supportive.{01}


Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Carbetocin (Systemic).

Before using this medication
»   Conditions affecting use, especially:
Allergy to oxytocin or carbetocin

Pregnancy—Carbetocin must not be used prior to delivery of the infant; use during pregnancy may result in hyperstimulation of the uterus, tumultuous labor, uterine rupture, cervical and vaginal lacerations, postpartum hemorrhage, uteroplacental hypoperfusion and deceleration of the fetal heart rate, fetal hypoxia, hypercapnea, or death
Other medical problems, especially vascular disease

Proper use of this medication
» Proper dosing


Side/adverse effects
Signs of potential side effects, especially abdominal pain, flushing, headache, hypotension, pruritus, tremor, anemia, anxiety, chest pain, chills, dyspnea, pain, and tachycardia


General Dosing Information
Carbetocin should not be administered prior to the delivery of the infant.{01}

Carbetocin has a long duration of action compared with oxytocin. Therefore, once uterine contractions have started, they cannot be stopped by discontinuing the medication.{01}

Although carbetocin may be administered before or after delivery of the placenta, if it is administered before, partial retention or trapping of the placenta theoretically could occur. However, no cases have been reported.{01}

If a single dose of carbetocin is not sufficient to induce adequate uterine contractions, more aggressive treatment with ergotamine or higher doses of oxytocin is recommended. Additional carbetocin should not be administered.{01}

If persistent bleeding occurs, the possibility of coagulopathy, retained placental fragments, or trauma to the genitourinary tract should be explored.{01}


Parenteral Dosage Forms

CARBETOCIN INJECTION

Usual Adult Dose
Atony, uterine (treatment) or
Hemorrhage, postpartum (treatment)
Single intravenous bolus injection, 100 micrograms over 1 minute following the delivery of the infant(s) by cesarean section under epidural anesthetic{01}


Strength(s) usually available
U.S.—
Not commercially available.

Canada—


100 mcg per mL (Rx) [Duratocin ( sodium chloride 9 mg) (glacial acetic acid (6–14 mcg) (water for injection ){01}]

Packaging and storage:
Store under refrigeration 2 to 8 °C (36 to 46 °F). Do not freeze. Once opened, carbetocin should be used immediately{01}



Developed: 08/07/2000



References
  1. Product Information: Duratocin(R), carbetocin. Ferring Pharmaceuticals, Toronto, Canada (PI revised 7/2000) reviewed 7/2000.
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