Registered Trademark of Richmond Veterinaria S.A.
Diazepam 5 mg | mL
Dazam. Tranquilizer and psychotropic/Benzodiazepine.
Use in Dogs, Cats and Sporting Horses.
Diazepam is a minor tranquilizer that depresses the limbic system, thalamus and hypothalamus, inducing a mild calming effect. It stimulates the benzodiazepine receptors in the CNS, which enhances the inhibitory action of GABA and potentiates the activity of CNS depressant neurotransmitters. It produces muscle relaxation at the spinal cord level by decreasing polysynaptic reflex activity and has anticonvulsant properties in most animals, raising the threshold for seizures.
The main route of administration is IV. It is important to emphasize that an effective non parenteral alternative is the IR route for the treatment and control of seizures in the Epileptic Ictus. This is because the hemorrhoidal veins drain into the circulatory system without passing through the liver, thus circumventing its first-step effect.
Continuous intravenous infusion of diazepam is not recommended because of the possibility of precipitation of diazepam in the parenteral solutions and its adsorption to the plastic of the infusion tube and bag.
Diazepam is highly liposoluble and is widely distributed throughout the body. It acts on specific receptors located in the post-synaptic nerve endings located in the CNS. The highest concentration of receptors is in the cerebral cortex, and to a lesser extent in the hypothalamus, cerebellum, midbrain, hippocampus and spinal cord.
It is metabolized in the liver through various pathways, such as demethylation, hydroxylation and glucuronic conjugation to various metabolites (nordiazepam, temazepam and oxazepam) all pharmacologically active. The conjugated metabolites are excreted especially in the urine and a small proportion in the bile.
The half-life of Diazepam and its metabolites in serum has been calculated as:
– Dogs: Diazepam 2, 5 – 3, 2 Hs. Nordiazepam 3 Hs.
– Cats: Diazepam 5, 5 Hs. Nordiazepam 21, 3 Hs.
– Horses: Diazepam 7 – 22 Hs.
Benzodiazepines have high plasma protein binding and diazepam has been reported to have more than 90% binding in several species.
Benzodiazepines and their metabolites are distributed in milk and may cause effects in the CNS of neonates.
Each 100 mL contains: Diazepam 500 mg; Excipients q.s. 100 mL.
Indications of Use
Dazam is a minor tranquilizer and its use is indicated as a tranquilizer, sedative, anxiolytic, central muscle relaxant, anticonvulsant and appetite stimulant.
It is used in combination with other drugs in the premedication, induction and maintenance of a balanced anesthesia.
Diazepam can be crystallized in parenteral solutions and adsorbed onto PVC tubing.
Applied slowly when given intravenously, a rapid injection in small animals and neonates can cause cardiotoxicity due to the propylene glycol present in its formulation.
Avoid application in small veins (may cause thrombophlebitis).
Keep out of reach of children and pets.
Diazepam is contraindicated in the following cases:
Not to be administered to horses intended for human consumption.
- – Liver or kidney disease.
- – Closed-angle glaucoma.
- – Neonates.
- – Respiratory depression.
- – Coma.
- – Shock.
- – Cats poisoned with organophosphates.
- – Very weakened animals.
In horses Diazepam can cause muscle twitching, respiratory depression and ataxia.
Sometimes cats exhibit idiosyncratic behavioural reactions of hyperactivity. This could be due to the release of overt anxiety that releases the behavioural inhibition that kept the cat treatable.
They can cause bradycardia and severe hypotension after rapid IV administration.
Interaction with other drugs
Benzodiazepines enhance the action of other CNS depressants. Diazepam exhibits extensive binding to plasma proteins and should be administered with caution with other drugs that also have high binding to plasma proteins. They should be given with caution in animals receiving cimetidine, because this drug impairs the oxidation of diazepam by the action of liver microsomal enzymes, which prolongs its half-life, and therefore, delays its elimination. The metabolism of diazepam can be altered by co-administration with fluoxetine, erythromycin, isoniazid, ketoconazole, propanolol, metroprolol and valproic acid. It increases the risk of poisoning in patients treated with digoxin.
Dogs and cats:
Anxiolytic, tranquilizing, pre-anesthetic and myorelaxant:
Both species at a rate of 0.2 – 0.4 mg/kg which corresponds to 0.4 – 0.8 mL per 10 kg. If necessary, the application can be repeated 2 to 3 times every 6 to 8 hours.
A dose of 0,5 to 1 mg/kg is recommended, corresponding to 1 to 2 mL every 10 kg, using a slow bolus intravenous route as the main route. The intra-rectal route can be used at a dose of 1 – 2 mg/kg which corresponds to 2 to 4 mL every 10 kg, as an alternative. In case of status epilepticus, the dose can be repeated in intervals of 5 – 10 minutes. Maximum 3 doses.
Oxygen in cats:
In doses of 0.05 – 0.4 mg/kg, which corresponds to 0.01 to 0.8 mL/kg IV for anorexic patients and for the treatment of behavioural problems.
Anesthetic induction and maintenance:
In dogs and cats at a dose of 0.2 – 0.4 mg/kg which corresponds to 0.4 to 0.8 mL every 10 kg, intravenously, followed by Ketamine 11 mg/kg intravenously. The duration of anesthesia is 5 to 22 minutes; recovery is characterized by 10 to 15 minutes of ataxia and incoordination. This dose is considered for a safe premedication, and can be increased up to 0.6 mg/kg which corresponds to 1.2 mL every 10 kg taking into account the age of the animal and its cardiac functioning.
The IM route is not recommended since it can be erratic.
It may precipitate in the syringe if mix with other drugs.
Its use is exclusive IV.
0,05 – 0,2 mg/kg IV corresponding to 1 – 4 mL per 100 kg.
Induction and Maintenance:
Xylazine – Diazepam – Ketamine 0.5 – 1 mg/kg – 0.2 mg/kg – 1.5 – 2 mg/kg.
Foals: 0.05 – 0.4 mg/kg IV. This corresponds to 1 – 8 mL per 100 kg.
Adults: 25 – 50 mg total IV. This corresponds to 5 – 10 mL total. Repeat in 30 minutes if necessary.
Treatment of intoxication: Flumazenil is a drug that reverses the effects of benzodiazepines (0.01 – 0.02 mg/kg IV). Flumazenil has a relatively short action (about 60 minutes), which may require repeated administration.
Store between 15 and 30°C, out of direct sunlight, in a dry and hygienic place. Keep out of reach of children and pets. Always consult your veterinarian.
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Grand Bourg, Buenos Aires, Argentina.