Alfentanil

Brands/Trade Names of Alfentanil in Kenya:

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Alfentanil in Kenya: Chemical Structure,use,abuse,Price,Brands
Alfentanil Chemical Structure

Mode of Action

Alfentanil is a synthetic short-acting opioid with analgesic and local anesthesia enhancing activity. Alfentanil primarily binds to mu-opioid receptor, a G-protein-coupled receptor, thereby mimicking the actions of morphine, the prototypical mu receptor agonist.

INDICATIONS

In adults, as an opioid analgesic supplement for use before and during anaesthesia.

It is indicated for:

• Short procedures and outpatient surgery.

• Procedures of medium and long duration when given as a bolus followed by supplemental doses or by continuous infusion.

At very high doses, Alfentanil may be used in adults as an anaesthetic induction agent in ventilated patients.

Alfentanil is indicated for use in neonates, infants, children and adolescents as:

• an opioid analgesic in association with a hypnotic to induce anaesthesia

• an opioid analgesic in association with general anaesthesia and for both short and long surgical procedures

DOSAGE AND ADMINISTRATION

Prior to starting treatment with opioids, a discussion should be held with patients to put in place a strategy for ending treatment with alfentanil in order to minimise the risk of addiction and drug withdrawal syndrome

Adults

Alfentanil 5 mg/ml solution for injection should be diluted with sodium chloride intravenous infusion BP, glucose intravenous infusion BP, or compound sodium lactate intravenous infusion BP (Hartmann’s solution). Such dilutions are compatible with plastic bags and giving sets. These dilutions should be used within 24 hours of preparation.

The recommended initial infusion rate for mechanically ventilated adult patients is 2 mg per hour (equivalent to 0.4 ml per hour) of undiluted Alfentanil 5 mg/ml solution for injection. For a 70 kg patient, this corresponds to approximately 30 micrograms per kilogram per hour.

Paediatric patients

Alfentanil 5 mg/ml solution for injection is not recommended for use in children in intensive care

CONTRAINDICATIONS

Hypersensitivity to the active substance, to other opioids, or to any of the excipients .

Obstructive airway disease or respiratory depression if not ventilating.

Concurrent administration with monoamine oxidase inhibitors or within 2 weeks of their discontinuation.

Administration in labour or before clamping of the cord during Caesarian section due to the possibility of respiratory depression in the new-born infant.

DRUG INTERACTIONS

Drugs modifying the effect of alfentanil

Sedative medicines such as benzodiazepines or related drugs

The concomitant use of opioids with sedative medicines such as benzodiazepines or related drugs increases the risk of sedation, respiratory depression, coma and death because of additive CNS depressant effect. The dose and duration of concomitant use should be limited .

Other Central Nervous System (CNS) depressants

Drugs such as barbiturates, neuroleptics, general anaesthetics and other non-selective CNS depressants (e.g. alcohol) may enhance or prolong the respiratory depressant effects of opioids. If other narcotic or CNS depressant drugs are used concurrently with alfentanil, the effects of the drugs can be expected to be additive. When patients have received such drugs, the dose of alfentanil required will be less than usual. Concomitant use with Alfentanil 5 mg/ml solution for injection in spontaneously breathing patients may increase the risk of respiratory depression, profound sedation, coma, and death.

Effect of Alfentanil on other drugs

Following the administration of alfentanil, the dose of other CNS-depressant drugs should be reduced. This is particularly important after surgery, because profound analgesia is accompanied by marked respiratory depression, which can persist or recur in the postoperative period. Administration of a CNS depressant, such as a benzodiazepine, during this period may disproportionally increase the risk for respiratory depression (see above).

In combination with alfentanil, the blood concentrations of propofol are 17% higher than in the absence of alfentanil. The concomitant use of alfentanil and propofol may require a lower dose of Alfentanil 5 mg/ml solution for injection.

Cytochrome P450 3A4 (CYP3A4) inhibitors

Alfentanil is metabolised mainly via the human cytochrome P450 3A4 enzyme. In vitro data suggest that potent cytochrome P450 3A4 enzyme inhibitors (e.g., ketoconazole, itraconazole, ritonavir) may inhibit the metabolism of alfentanil. Available human pharmacokinetic data indicate that the metabolism of alfentanil is inhibited by fluconazole, voriconazole, erythromycin, diltiazem and cimetidine (known cytochrome P450 3A4 enzyme inhibitors). This could increase the risk of prolonged or delayed respiratory depression. The concomitant use of such drugs requires special patient care and observation; in particular, it may be necessary to lower the dose of Alfentanil 5 mg/ml solution for injection.

Treatment with drugs which may depress the heart or increase vagal tone, such as beta-blockers and anaesthetic agents, may predispose to bradycardia or hypotension. Bradycardia and possibly cardiac arrest can occur when Alfentanil 5 mg/ml solution for injection is combined with non-vagolytic muscle relaxants.

Monoamine Oxidase Inhibitors (MAOI)

It is usually recommended to discontinue MAO-inhibitors 2 weeks prior to any surgical or anaesthetic procedure.

Serotonergic drugs

Coadministration of alfentanil with a serotonergic agent, such as Selective Serotonin Reuptake Inhibitors (SSRIs), Serotonin Norepinephrine Reuptake Inhibitors (SNRIs), or Monoamine Oxidase Inhibitors (MAOIs), may increase the risk of serotonin syndrome, a potentially life-threatening condition.

ADVERSE EFFECTS

Gastrointestinal: nausea ,vomiting

Cardiovascular: arrhythmia, bradycardia ,hypertension ,hypotension ,tachycardia

Musculoskeletal: chest wall rigidity ,skeletal muscle movements

Respiratory: apnea, postoperative respiratory depression

Central Nervous System: blurred vision, dizziness, sleepiness/postoperative sedation

Reporting of suspected adverse reactions:

The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org or clicking below button:


Alfentanil in Kenya
Alfentanil in Kenya
Alfentanil in Kenya
Alfentanil in Kenya
Alfentanil in Kenya
Alfentanil in Kenya

Clinical | Pharmacokinetic data


Pregnancy Category: C
Routes of Administration: Intravenous; Subcutaneous
Bioavailability: ~50%
Protein Binding: 92%
Metabolosim: Hepatic
Onset of Action: Immediate
Elimination Half life: 90–111 minutes
Excretion: via urine

Legal Status | Dosage forms & Strengths


Prescription Category:
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This is a controlled Schedule 1 Drug ,Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:
Injectable

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