Gospas

Gospas Uses, Dosage, Side Effects, Food Interaction and all others data.

An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.

Chlordiazepoxide has antianxiety, sedative, appetite-stimulating and weak analgesic actions. The drug seems to block EEG arousal from stimulation in the brain stem reticular formation. The drug has been studied extensively in many species of animals and these studies are suggestive of action on the limbic system of the brain, which recent evidence indicates is involved in emotional responses. Hostile monkeys were made tame by oral drug doses which did not cause sedation. Chlordiazepoxide revealed a "taming" action with the elimination of fear and aggression. The taming effect of chlordiazepoxide was further demonstrated in rats made vicious by lesions in the septal area of the brain. The drug dosage which effectively blocked the vicious reaction was well below the dose which caused sedation in these animals.

Cilnidipine acts on the L-type calcium channels of blood vessels by blocking the incoming calcium and suppressing the contraction of blood vessels, thereby reducing blood pressure. Cilnidipine also works on the N-type calcium channel located at the end of the sympathetic nerve, inhibiting the emission of norepinephrine and suppressing the increase in stress blood pressure.

Administration of cilnidipine has been shown to present an antisympathetic profile in vitro and in vivo. It decreases blood pressure safely and effectively without excessive blood pressure reduction or tachycardia.

Gospas
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Gospas
Generic	Cilnidipine + Chlordiazepoxide + Dicycloverine / Dicyclomine
Weight	2.5mg
Type	Tablet
Therapeutic Class
Manufacturer	Dr Reddys Laboratories Ltd
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

Chlordiazepoxide is a benzodiazepine used to treat the withdrawal symptoms of acute alcoholism, to treat preoperative anxiety, and to treat anxiety over a short term period.

For the management of anxiety disorders or for the short-term relief of symptoms of anxiety, withdrawal symptoms of acute alcoholism, and preoperative apprehension and anxiety.

Cilnidipine is used for the management of hypertension for end-organ protection. It is reported to be useful in elderly patients and in those with diabetes and albuminuria. Cilnidipine has been increasingly used in patients with chronic kidney disease.

Hypertension is the term used to describe the presence of high blood pressure. The blood pressure is generated by the force of the blood pumped from the heart against the blood vessels. Thus hypertension is caused when there is too much pressure on the blood vessels and this effect can damage the blood vessel

Gospas is also used to associated treatment for these conditions: Alcohol Withdrawal Syndrome, Anxiety, Anxiety Disorders, Depression, Peptic Ulcer Disease, Acute Anxiety, Pyschosomatic diseaseHigh Blood Pressure (Hypertension)

How Gospas works

Chlordiazepoxide binds to stereospecific benzodiazepine (BZD) binding sites on GABA (A) receptor complexes at several sites within the central nervous system, including the limbic system and reticular formation. This results in an increased binding of the inhibitory neurotransmitter GABA to the GABA(A) receptor. BZDs, therefore, enhance GABA-mediated chloride influx through GABA receptor channels, causing membrane hyperpolarization. The net neuro-inhibitory effects result in the observed sedative, hypnotic, anxiolytic, and muscle relaxant properties.

Dosage

Gospas dosage

5-10 mg once daily, increase to 20 mg once daily if necessary.

Side Effects

Dizziness; flushing; headache; hypotension; peripheral oedema; tachycardia; palpitations; GI disturbances; increased micturition frequency; lethargy; eye pain; depression; ischaemic chest pain; cerebral or myocardial ischaemia; transient blindness; rashes; fever; abnormal liver function; gingival hyperplasia; myalgia; tremor; impotence.

Toxicity

LD₅₀=537 mg/kg (Orally in rats). Signs of overdose include respiratory depression, muscle weakness, somnolence (general depressed activity).

The percentage of reports of cilnidipine that express drug toxicity reported as side effects are 5.26%.

Precaution

Hypotension, poor cardiac reserve, heart failure. Sudden withdrawal may exacerbate angina. Discontinue in patients who experience ischemic pain following administration. Pregnancy, lactation.

Interaction

Other antihypertensives; aldesleukin; antipsychotics that cause hypotension; may modify insulin and glucose responses; quinidine; carbamazepine; phenytoin; rifampicin; cimetidine; erythromycin.

Volume of Distribution

Drugs on the group of dihydropyridines such as cilnidipine tend to have a large volume of distribution.

Elimination Route

Cilnidipine presents a very rapid absorption with a maximum peaked concentration after 2 hours. Its distribution tends to be higher in the liver as well as in kidneys, plasma and other tissues. Cilnidipine does not present a high accumulation in the tissue after repeated oral administration.

Cilnidipine is reported to present very low bioavailability determined to be approximately 13%. This low bioavailability is suggested to be due to its low aqueous solubility and high permeability. Hence, efforts have been made in order to find an innovative formulation that can significantly improve the bioavailability of this drug. One of these formulations corresponds to the generation of polymeric nanoparticles which enhance the bioavailability by 2.5-3-fold.

Half Life

24-48 hours

The half-life of the hypotensive effect for cilnidipine is of about 20.4 min.

Elimination Route

Chlordiazepoxide is excreted in the urine, with 1% to 2% unchanged and 3% to 6% as conjugate.

Cilnidipine gets eliminated through the urine in a proportion of 20% of the administered dose and 80% is eliminated by the feces.

Pregnancy & Breastfeeding use

No specific information about USFDA pregnancy category. Caution should be exercised during Cilnidipine use in pregnancy. Nursing mothers should consult a physician before taking Cilnidipine.