Description
Latin name
Diprivan
Release form
Emulsion for intravenous administration.
Packing
in ampoules of 20 ml in a pack of cardboard 5 pcs.
Pharmacological action
Dynamic – a drug for the treatment of erectile dysfunction. Under the conditions of sexual stimulation, it restores impaired erectile function by increasing blood flow in the penis.
The physiological mechanism of erection involves the release of nitric oxide (NO) in the cavernous body due to sexual arousal. NO activates the enzyme guanylate cyclase, which leads to an increase in the concentration of cGMP. In turn, cGMP causes relaxation of the smooth muscles of blood vessels and, accordingly, the flow of blood into the cavernous body of the penis.
Sildenafil is a selective inhibitor of cGMP-specific type 5 phosphodiesterase (PDE5), which causes the breakdown of cGMP in the cavernous body of the penis. It does not have a direct relaxing effect on the smooth muscles of the cavernous body, but enhances the relaxing effect of NO and increases blood flow in the penis. Upon activation of the NO cGMP chain observed during sexual stimulation, inhibition of PDE5 leads to an increase in the level of cGMP in the cavernous body. The pharmacological effect is achieved only in the presence of sexual stimulation.
The activity of sildenafil in relation to PDE5 is superior to activity against other known phosphodiesterase isoenzymes: PDE6 – 10 times, PDE1 – more than 80 times PDE2 PDE4, PDE7 PDE11 – more than 700 times. Sildenafil is 4,000 times more selective for PDE5 compared to PDE3, which is of great importance, since PDE3 is one of the key enzymes in the regulation of myocardial contractility. having a short-term effect and causing the rapid onset of drug sleep for about 30 seconds.
Usually recovery of consciousness occurs quickly.
Indications
water anesthesia
maintenance of anesthesia
providing a sedative effect in patients who undergo mechanical ventilation with intensive therapy
ensuring a sedative effect with preservation of consciousness during diagnostic procedures and surgical interventions.
Contraindications
Hypersensitivity.
Pregnancy and lactation
Diprivan should not be used during pregnancy, but the drug is used during termination of pregnancy in the first trimester as a means for general anesthesia.
Propofol crosses the placental barrier and can cause neonatal depression, so the drug should not be used in obstetric practice as an anesthetic.
When using Diprivan in the mother during breastfeeding, safety for the baby was not established.
Composition of
1 ml of the emulsion contains propofol 10 mg
reaction: as a rule: Induction anesthesia runs smoothly, with minimal signs of arousal. During induction, depending on the dose and on the means used for sedation, hypotension and temporary apnea may occur. Hemodynamic parameters usually remain stable while maintaining anesthesia.
Other side effects during induction of anesthesia, the period of its maintenance and recovery rarely occur.
Rare cases of epileptiform movements, including convulsions and opistotonus, have been reported. Pulmonary edema was observed.
During awakening, only a small number of patients have nausea, vomiting, and headache. After prolonged use of Diprivan, cases of discoloration of urine were sometimes observed.
In very rare cases, after the administration of Diprivan, there are clinical signs of anaphylaxis, which include bronchospasm, angioedema, erythema and hypotension. In some cases, postoperative fever. As with other anesthetics, sexual disinhibition may occur.
When prescribing Diprivan in doses of more than 4 mg / kg / h, isolated cases of rhabdomyolysis have been reported.
Local reactions: rarely – thrombosis and phlebitis at the injection site.
Drug Interaction
Diprivan is well combined with spinal and epidural anesthesia with medications used for premedication with muscle relaxants and analgesics.
In cases where general anesthesia is used as an adjunct to the methods of regional anesthesia used, Diprivan may be used in smaller doses than usual.
With the use of Diprivan with heart rate-reducing agents, the risk of developing pronounced bradycardia is increased.
No pharmacological compatibility noted.
Diprivan should not be mixed with any other injectable or infusion solution before administration except for 5% dextrose in PVC bags or glass infusion bottles, lignocaine for injection or alfentanil for injection in plastic syringes.
When administering muscle relaxants, atracurium besylate and mivacurium chloride should not use the same infusion line as for Diprivan without first washing it.
Overdose
Symptoms: An accidental overdose can probably cause cardiac arrest and breathing.
Treatment: In case of respiratory depression, ventilation with oxygen should be performed. At suppression of cardiovascular activity the head of the patient should be lowered, and, if necessary, to use plasma substitutes and vasopressor means.
Storage conditions
Store at 2 ° to 25 ° C and do not freeze.
Expiration
3 years.
Deystvuyuschee substances
Propofol
dosage form
dosage form
infusion emulsion
AstraZeneca, Britain
