FENTANYL (Phentanylum; joint venture. A) — narcotic analgetic. 1 (2-Fe-nilztil) - 4 - (N-propionilfenilami-but) - piperidine; C22H28N20:
White crystal powder. It is almost water-insoluble. It is easily alcohol-soluble.
Apply in the form of citrate — Phen-tanyli Citras (a synonym; Fentanil, Fenta-nest, Sentonyl, Sublimaze, etc.).
On analgetic activity in experimental conditions F. surpasses morphine (see) by 200 — 400 times. According to a wedge, to observations analgetic activity F. is also much higher, than at morphine. The analgesic effect arises in
1 — 2 min. after intravenous administration of F. Analgeziya after single introduction is observed within 20 — 30 min. Further during nek-ry time (sometimes till several o'clock) decrease in painful sensitivity can be noted. At intramuscular or hypodermic introduction the effect occurs in
5 — 12 min. F. it is soaked up from intestines, however at the same time for achievement of an analgesia higher doses are necessary, than at parenteral administration.
Short duration of effect F. it is caused by bystry metabolism of connection, and also its redistribution in an organism. Biotransformation F. there is a hl. obr. in a liver. It is allocated with kidneys and through went. - kish. a path preferential in the form of metabolites and partially — in not changed look.
T. can cause respiratory depression up to its stop. Respiratory depression begins to be shown after its intravenous administration in a dose of 0,2 — 0,3 mg. In doses of St. 0,5 — 0,6 mg drug can cause an apnoea.
T. does not exert the significant oppressing effect on contractility of a myocardium. At administration of drug the urezheniye of a rhythm of cordial reductions is observed, expressiveness to-rogo depends on its dose. Bradycardia is followed by increase in duration of an interval P — R on an ECG. For easing or the prevention caused F. bradycardia use atropine (see). The hypotensive effect is observed at introduction of rather high doses of drug and develops usually against the background of the expressed bradycardia. Hypotension is not eliminated with introduction of holinoblokator and antihistaminic means. On its background the hypertensive effect of adrenaline remains. Caused F. decrease in the ABP is recovered after introduction of Nalorfinum (see) or Naloxonum (see).
Like morphine, T. exerts the stimulating impact on unstriated muscles of intestines and bronchial tubes. M-ho-linoblokatory and specific antagonists of narcotic analgetics partially or completely eliminate these effects.
Emetic action at F. it is expressed poorly. Causes narrowing of pupils in people and dogs; the mydriasis is characteristic of mice, cats, monkeys. In high doses raises a muscle tone that in a wedge, conditions can be shown by muscle tension of a thorax and stomach.
T. apply as an anesthetic. For premedication before an anesthesia (see) it enter in doses 0,05 — 0,1 mg (1 — 2 ml of 0,005% of solution intramusculary) in 30 min. prior to an anesthesia. For a neyroleptanalgeziya (see) F. enter at the rate of 0,05 mg (1 ml of 0,005% of solution) for 5 kg of the weight (weight) of a body together with Droperidolum (see) or other active neuroleptics. For maintenance of an analgesia enter every 10 — 30 min. on 1 — 3 ml 0,005% of solution.
At the short extracavitous operations performed without use of kurarepodobny means, T. apply at the rate of 0,05 mg on 10 — 20 kg of the weight (weight) of a body. At the same time it is necessary to provide an opportunity in case of need to carry out an intubation of a trachea and an artificial respiration. At operations under local anesthesia (see Anesthesia local) F. it can be used as additional anesthetic in doses of 0,025 — 0,05 mg intravenously or intramusculary.
T. apply also to stopping of acute pains at a myocardial infarction, renal and hepatic gripes. For this purpose it is entered intravenously or intramusculary
1 — 2 ml of 0,005% of solution (it is frequent in a combination with neuroleptics).
At use F. side effects can be observed: respiratory depression, motive excitement (see Excitement psychomotor), muscle tension of a thorax and extremities (see the Tone), a bronchospasm (see), hypotension (see Hypotension arterial), a sinus bradycardia (see).
It is contraindicated at Cesarean section (before extraction of a fruit) and other obstetric operations in connection with high sensitivity of a respiratory center of a fruit to the oppressing action F., and also at the expressed hypertensia in a small circle of blood circulation, oppression of a respiratory center, pneumonia, an atelectasis and a heart attack of a lung, bronchial asthma, tendency to a bronchospasm, extrapyramidal disturbances.
The patient receiving insulin, corticosteroids or antihypertensives, T. it is necessary to enter in the reduced doses.
At repeated use of drug can develop accustoming (see Accustoming to pharmaceuticals) and medicinal dependence (see).
Forms of release: ampoules on 2 and
10 ml of 0,005% of solution, bottles on 10 ml of 0,005% of solution. Storage: in the place protected from light.
Issue and use F. it is made according to the rules established for morphine and other narcotic analgetics.
See also Analgezirtsyushchy environments - with t in and.
Bibliography: D and r and N I am T. M N. To it -
a roleggtayalgeziya, M., 1969; To at -
z p M. I. N, Yefimova N. V. and About with and p about in and N. A. Neyroleptanalge-ziya in surgery, M., 1976; G a r d about -
<• k i J. F. a. Y e 1 p about sky J.
A study of some of the pharmacologic actions of ten-tanyl citrate, Toxicol, appl. Pharmacol., v. G, j). 48, 1964; J a n s s e n P. A. J., N i e m e g e e of s C. J. E. a. D o-Ti y J. G. H. The inhibitory effect of Fe'ntanyl and other morphine-like analgesics on the warm water induced tail withdrawal reflex in rats, Arzneimittel-Forsch., S. 502, 1963; Y e 1 n o s to at J. a. G a r-docky J. F. A study "of some of the pharmacologic actions of fentanyl citrate and droperidol, Toxicol, appl. Pharmacol.,
v. 6, p. 63, 1964. V. V. Churyunanov.