Azaperone
Encyclopedia
Azaperone is a pyridinylpiperazine
and butyrophenone
neuroleptic drug
with sedative
and antiemetic
effects, which is used mainly as a tranquilizer
in veterinary medicine. It is used mainly in pigs and elephants. More rarely it may be used in humans as an antipsychotic
drug, but this is uncommon. Use in horses is avoided as adverse reactions may occur.
Azaperone acts primarily as a dopamine
antagonist but also has some antihistaminic
and anticholinergic
properties as seen with similar drugs such as haloperidol
. Azaperone may cause hypotension
and while it has minimal effects on respiration in pigs, high doses in humans can cause respiratory depression which may be why it is rarely used in humans.
The most common use for azaperone is in relatively small doses to reduce aggression in farmed pigs, either to stop them fighting or to encourage sows to accept piglets. Higher doses are used for anesthesia
in combination with other drugs such as xylazine
, tiletamine
and zolazepam
. Azaperone is also used in combination with strong narcotics such as etorphine
or carfentanil
for tranquilizing large animals such as elephants.
Pyridinylpiperazine
1-piperazine is a chemical compound and piperazine derivative. Some derivatives of this substance are known to act as potent and selective a2-adrenergic receptor antagonists, such as 1-piperazine....
and butyrophenone
Butyrophenone
Butyrophenone is a chemical compound ; some of its derivatives are used to treat various psychiatric disorders such as schizophrenia, as well as acting as antiemetics....
neuroleptic drug
Drug
A drug, broadly speaking, is any substance that, when absorbed into the body of a living organism, alters normal bodily function. There is no single, precise definition, as there are different meanings in drug control law, government regulations, medicine, and colloquial usage.In pharmacology, a...
with sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
and antiemetic
Antiemetic
An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer....
effects, which is used mainly as a tranquilizer
Tranquilizer
A tranquilizer, or tranquilliser , is a drug that induces tranquility in an individual.The term "tranquilizer" is imprecise, and is usually qualified, or replaced with more precise terms:...
in veterinary medicine. It is used mainly in pigs and elephants. More rarely it may be used in humans as an antipsychotic
Antipsychotic
An antipsychotic is a tranquilizing psychiatric medication primarily used to manage psychosis , particularly in schizophrenia and bipolar disorder. A first generation of antipsychotics, known as typical antipsychotics, was discovered in the 1950s...
drug, but this is uncommon. Use in horses is avoided as adverse reactions may occur.
Azaperone acts primarily as a dopamine
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
antagonist but also has some antihistaminic
Histamine
Histamine is an organic nitrogen compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter. Histamine triggers the inflammatory response. As part of an immune response to foreign pathogens, histamine is produced by...
and anticholinergic
Choline
Choline is a water-soluble essential nutrient. It is usually grouped within the B-complex vitamins. Choline generally refers to the various quaternary ammonium salts containing the N,N,N-trimethylethanolammonium cation....
properties as seen with similar drugs such as haloperidol
Haloperidol
Haloperidol is a typical antipsychotic. It is in the butyrophenone class of antipsychotic medications and has pharmacological effects similar to the phenothiazines....
. Azaperone may cause hypotension
Hypotension
In physiology and medicine, hypotension is abnormally low blood pressure, especially in the arteries of the systemic circulation. It is best understood as a physiologic state, rather than a disease. It is often associated with shock, though not necessarily indicative of it. Hypotension is the...
and while it has minimal effects on respiration in pigs, high doses in humans can cause respiratory depression which may be why it is rarely used in humans.
The most common use for azaperone is in relatively small doses to reduce aggression in farmed pigs, either to stop them fighting or to encourage sows to accept piglets. Higher doses are used for anesthesia
Anesthesia
Anesthesia, or anaesthesia , traditionally meant the condition of having sensation blocked or temporarily taken away...
in combination with other drugs such as xylazine
Xylazine
Xylazine is a drug that is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals. An analogue of clonidine, it is an agonist at the α2 class of adrenergic receptor....
, tiletamine
Tiletamine
Tiletamine is a dissociative anesthetic and pharmacologically classified as an NMDA receptor antagonist. It is related chemically and pharmacologically to other anesthetics in this family such as ketamine and phencyclidine...
and zolazepam
Zolazepam
Zolazepam was discoverd by a team at Parke-Davis in the 1960s. is a pyrazolodiazepinone derivative structurally related to the benzodiazepine drugs, which is used as an anaesthetic for a wide range of animals in veterinary medicine...
. Azaperone is also used in combination with strong narcotics such as etorphine
Etorphine
Etorphine is a semi-synthetic opioid possessing an analgesic potency approximately 200 times that of morphine. It was first prepared in 1960 from oripavine, which does not generally occur in opium poppy extract but rather in "poppy straw" and in related plants, Papaver orientale and Papaver...
or carfentanil
Carfentanil
Carfentanil or carfentanyl is an analogue of the popular synthetic opioid analgesic fentanyl, and is one of the most potent opioids known . Carfentanil was first synthesized in 1974 by a team of chemists at Janssen Pharmaceutica which included Paul Janssen...
for tranquilizing large animals such as elephants.