Benzoctamine: uses and side effects of this drug
Anti-anxiety drugs are used to treat symptoms or conditions such as anxiety. In this article we will know a relatively new drug, which has sedative and anxiolytic properties, and which also does not depress the respiratory system: benzoctamine .
We will know its composition, its mechanism of action, indications, side effects and studies carried out.
Benzoctamine: general characteristics
Benzoctamine is a drug with sedative and anxiolytic properties . It is a relatively new drug, although its popularity is increasing as it can have comparable sedative and anti-anxiety effects to other drugs without its potentially fatal respiratory depressive side effects.
It is marketed under the name “Tacitin”. It’s a little different from most sedative medications, because in most clinical trials it doesn’t produce respiratory depression, and it actually stimulates the respiratory system.
Thus, when compared to other sedative and anti-anxiety medications such as benzodiazepines (such as diazepam), is a safer medication when it comes to reducing anxiety or calming down .
However, it should be noted that when benzoctamine is given in conjunction with other drugs that cause respiratory depression (such as morphine), it may cause an increase in respiratory depression.
Compound
Chemically, benzoctamine belongs to a group of compounds called dibenzobicyclooctodienes ; it is a tetracyclic compound formed by four rings that are configured three-dimensionally. This structure is closely related to that of the tetracyclic antidepressant maprotiline.
Indications
Benzoctamine is used for outpatient treatment of patients with anxiety, to control aggression, bedwetting, fear and mild social maladjustment in children.
So, his main indication is anxiety. The evidence suggests that is as effective as other medications for clinical anxiety, such as diazepam . Studies are mixed, with some suggesting that higher doses of benzoctamine are needed than diazepam to produce the same pharmacological effects. However, as we shall see, its side effects are partly less dangerous than those of most other sedatives.
In fact, the most important thing about this drug is that produces anxiolytic effects without producing the respiratory depression typical of other sedatives . In this way, benzoctamine became an alternative to benzodiazepines, which could also be used in patients with respiratory failure.
On the other hand, benzoctamine can also be used for the treatment of hypertension.
Pharmacokinetics
Benzoctamine can be given orally (in tablet form) or intravenously (injected directly into the blood). This makes the drug 100% available to the body through the intravenous route, and 90% available if administered orally.
When given orally, the dose is 10 mg three times a day; when given intravenously, patients receive benzoctamine at a rate of 5 mg/minute until 20 to 40 mg is injected.
It is metabolized by the liver, and its elimination half-life (the time it takes for the body to completely eliminate the substance) is between 2 and 3 hours. Its excretion is renal (it is excreted through the kidneys).
Effects
The anxiolytic effects of benzoctamine are similar to those of diazepam (another anxiolytic), but it differs from diazepam in that benzoctamine has antagonistic effects on epinephrine and norepinephrine, and even appears to reduce serotonin .
Relatively little is known about how it exerts its effects, but studies suggest that it is the reduction of serotonin, epinephrine and norepinephrine that (partially) causes benzoctamine’s pharmacological and behavioural effects.
Side effects
Some of the side effects of benzoctamine are drowsiness, dry mouth, headache and dizziness .
Studies
Animal studies have shown how sedative hypnotic drugs tend to cause dependence in animals, whereas benzoctamine has been shown not to cause addiction . In addition, other animal studies show how benzoctamine reduces blood pressure through the adrenergic system.
Bibliographic references:
- Maître, L., Staehelin, M., Bein, H. (1970). Effects of benzoctamine, a new psychoactive drug, on catecholamine metabolism. Biochemical pharmacology, 19(11): 2875-92.
- Sonó, H., Dale, M., Ritter, J.M. and Moore, P. (2003). Pharmacology (5. ed.). Edinburgh: Churchill Livingstone.
- Stahl, S.M. (2002). Essential Psychopharmacology. Neuroscientific bases and clinical applications. Barcelona: Ariel.