Barbiturate is a drug that acts as a central nervous system depressant, and can, therefore, produce a wide spectrum of effects, from mild sedation to total anesthesia. They are also effective as anxiolytics, hypnotics, and anticonvulsants. Barbiturates have addiction potential, both physical and psychological. They have largely been replaced by benzodiazepines in routine medical practice, particularly in the treatment of anxiety and insomnia, due to the significantly lower risk of addiction and overdose and the lack of an antidote for barbiturate overdose.
Types/ Classification of Barbiturate
| Barbiturates |
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Mechanism of action of Barbiturate
Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. Insufficiently high therapeutic doses, barbiturates induce anesthesia. Barbiturates bind at a distinct binding site associated with a Cl– ionopore at the GABAA receptor, increasing the duration of time for which the Cl– ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
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The effects of barbiturates on the number of cells expressing c-fos-like immunoreactivity (c-for-LI), a marker of neuronal activation, within lamina I, IIo of the trigeminal nucleus caudalis and the nucleus of the solitary tract 2 hours after the intracisternal injection of capsaicin (0.1 mL; 15.25 mg/mL) or vehicle in urethane-anesthetized guinea pigs (N = 45) /was examined/. Robust c-fos-LI was observed within nuclei of cells in the trigeminal nucleus caudalis after capsaicin (329 +/- 35). Barbiturates dose-dependently reduced the number of labeled cells to a maximum of 66% (1000 micrograms/kg intraperitoneally [i.p.], P < .01) in lamina I, IIo but not within area postrema, medial reticular nucleus, or the nucleus of the solitary tract. Pretreatment with bicuculline (30 micrograms/kg i.p.) blocked the effect of barbiturates, thereby suggesting the importance of the GABAA receptor to activation involved in the transmission of nociceptive information. Our studies suggest the possibility that GABAA receptors might provide an important therapeutic target in a pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।" data-rx-term="migraine" data-rx-definition="Migraine is a recurring headache disorder often with throbbing pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।">migraine and related headache disorders.
Indications of Barbiturate
- Typical applications for barbiturate are sedative, hypnotic for short-term, preanesthetic and control of convulsions in emergencies
- Status Epilepticus
- Sedation
- Insomnia
- Sleeplessness
- Severe Convulsion
- Withdrawal Symptoms
- Generalized seizure
- Partial onset seizure Epilepsy
- Barbituratealso has an application in reducing intracranial pressure in Reye’s syndrome, traumatic brain injury and induction of coma in cerebral ischemia patients.
- For the short-term treatment of insomnia.
- A headache
- A migraine
- A tension Headache
- Used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain.
Contra-Indications of Barbiturate
- Porphyria
- High blood pressure
- Heart disease
- Abnormally low blood pressure
- Pneumonia
- Lung failure causing loss of breath
- Decreased lung function
- Liver problems
- Periods of Not breathing
- Pregnancy
- Chronic obstructive lung disease
Side Effects
The most common
- Memory or concentration problems
- Excitement, irritability, aggression, or confusion
- Dizziness
- constipation
- muscle aches
- Nausea and vomiting
- Severe stomach ache
- diarrhea,
- anorexia,
- flatulence,
- a headache,
- dizziness,
- heartburn
- joint pain
Common
- Memory loss.
- Impaired attention span.
- Agitation.
- Depression.
- Nausea and vomiting
- Severe stomach ache
- Severe diarrhea
- Mouth sores
- Vaginal thrush
- Skin rash
- A headache
Rare/Less common
- Confusion
- Fever or sore throat
- Rash
- Slowed breathing or breathing difficulties
- Sores in the mouth
- Broken blood vessels under the skin
- Easy bruising or bleeding
- Swelling of the eyes, lips, or cheeks
- Blistering or peeling of the skin
- Restless muscle movements in the eyes, tongue, jaw, or neck
Drug Interactions
A barbiturate,may interact with following drugs, supplements & may change the efficacy of drug
- albendazole
- alcohol
- allopurinol
- alpha blockers (e.g., alfuzosin, doxazosin, silodosin, tamsulosin)
- amphetamines (e.g., dextroamphetamine, lisdexamphetamine)
- anti-cancer medications (e.g., cabazitaxel, docetaxel; doxorubicin; etoposide, ifosfamide, irinotecan, vincristine)
- antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- baclofen
- benzodiazepines (e.g., chlordiazepoxide, clonazepam, diazepam, lorazepam)
- beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
- bupropion
- calcitriol
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- carbamazepine
- carvedilol
- celecoxib
- ciprofloxacin
- clobazam
- oral corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
- cyclosporine
- doxycycline
- estrogens (e.g., conjugated estrogen, estradiol, ethinyl estradiol)
- folic acid
- gabapentin
- “gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
- lansoprazole
- loperamide
- losartan
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- multivitamins
- montelukast
- ondansetron
- phenytoin
- progestins (e.g., dienogest, levonorgestrel, medroxyprogesterone, norethindrone)
- proton pump inhibitors (e.g., lansoprazole, omeprazole)
- ranitidine
- selective serotonin reuptake inhibitors (SSRIs;e.g., citalopram, duloxetine, fluoxetine,paroxetine, sertraline)
- sildenafil
- “statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
- theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
- thiazide diuretics (e.g., chlorothiazide, hydrochlorothiazide)
- tramadol
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- valproic acid
- warfarin
- zafirlukast
References
