Spastone

Uses

Dicycloverine is used for:

• Functional bowel/ irritable bowel syndrome
• Urinary incontinence secondary to unstable detrusor muscle
• Infantile colic
• GIT spasm
• Colicky abdominal pain
• Diverticulitis
• Abdominal colic

Dimethicone is an ingredient used to treat dry and irritated eyes.

Dimethicone is a colorless liquid with both cosmetic and therapeutic uses. It is used in topical creams and ointments to help distribute the active ingredients. Dimethicone is used as an anti-foaming agent, a hair and skin conditioner, and in the treatment of head lice and, as an anti-bloating/anti-flatulence agent , .

Spastone is also used to associated treatment for these conditions: Functional bowel syndrome, Irritable Bowel Syndrome (IBS), Gastrointestinal cramps caused by GasAcute Diarrhoea, Aerophagy, Dry Skin, Duodenal Ulcer, Dyspepsia, Flatulence, Gastric Ulcer, Gastritis, Gastro-esophageal Reflux Disease (GERD), Hiatus Hernia, Pancreatic Insufficiency, Post Operative Gas, Pre-operative Gas, Stress Ulcers, Bowel preparation therapy, Carbohydrate Digestion, Digestive Aid, Fat Digestion, Protein Digestion

How Spastone works

Dicyclomine achieves its action partially through direct antimuscarinic activity of the M1, M3, and M2 receptors; and partially through antagonism of bradykinin and histamine. Dicyclomine non-competitively inhibits the action of bradykinin and histamine, resulting in direct action on the smooth muscle, and decreased strength of contractions seen in spasms of the ileum.

When applied topically, dimethicone forms a layer to delay the evaporation of water . In the treatment of head lice dimethicone 100, the respiratory systems of head lice are targeted. NYDA works by suffocating the lice, nymphs and the embryos. The physical properties of this drug, including the viscosity and spreading property of the solution allow it to easily flow into the respiratory system of all developmental stages of the insect, causing suffocation and death of the organisms. It diffuses through the stigmata (spiracles) of the lice, into the tracheae of the head lice as well as through the aeropyles of the egg operculum. The solution then displaces oxygen. The low viscosity, volatile dimethicone enables the NYDA head lice solution to penetrate into the breathing system. Its evaporation causes the thickening of the NYDA solution. The remaining high viscosity dimethicone ultimately encloses the respiratory system and thus leading to suffocation of all stages of head lice (adult lice, larvae and eggs). This mode of action prevents the development of lice resistance by preventing the formation of new progency .

Studies performed using house crickets and lice suggest a close correlation between the death of the lice and the influx of the solution into the insect head tracheae. These data strongly suggest that the total filling of the head tracheae immediately blocks the oxygen supply to the insect central nervous system. Death, following numerous stages of disability after the entrance of dimethicones into the abdominal tracheal system, demonstrates the sequence of oxygen deprivation. NYDA was applied directly to the head and mouth of the organism, and was found to have no effect when applied solely to the outside of the head/mouth .

Dosage

Spastone dosage

Oral dosage forms-

• Adults:10 to 20 mg three times a day.
• Children >6 months of age: 5 to 10 mg three times a day.
• Children <6 months of age: Dose must be determined by the doctor.

Oral dicycloverine Hydrochloride should be started as soon as possible

Intramuscular dosage form

• Adults:Intramuscular injection. Not for intravenous use. The recommended intramuscular dose is 80 mg daily (in 4 equally divided doses).

Intramuscular dosage form should not be used for periods longer than 1 or 2 days.

Side Effects

Insomnia, mydriasis, cycloplegia, increased ocular tension, urinary hesitancy, palpitations, dyspnea.

Toxicity

Patients experiencing an overdose may present with headache, nausea, vomiting, blurred vision, dilated pupils, dizziness, dry mouth, difficulty swallowing, CNS stimulation, as well as hot, dry skin. Treat patients with gastric lavage, emetics, activated charcoal, sedatives for excitement, and a cholinergic agent if indicated.

The oral LD₅₀ in mice is 625mg/kg.

The minimum lethal oral dose of dimethicone 200 (50 cs), dimethicone 550 (75 cs), dimethicone in rats .

A 76-week dietary toxicity study of a silicone antifoam compound (94% polydimethylsiloxane silicone oil and 6% silicone dioxide) was performed in mice. Three groups were given diet containing 0, 0.25%, or 2.5% of the test article. The dose levels in the treatment groups were estimated to be 580 and 5800 mg/kg/day. Mortality was increased in the 5800 mg/kg/day females. No target organs of toxicity were observed. The no-effect dose was 580 mg/kg/day. This study is of limited usefulness for assessing the toxicity of dimethicones, due to the small number of organs/tissues that were examined .

In one clinical study, 145 subjects were treated with either NYDA (dimethicone )or with a permethrin-based lice product. The number of subjects experiencing any adverse events was similar in both groups. In the NYDA group, 29 adverse events were reported in 25 subjects. All except two adverse events were categorized as being unrelated to the lice treatment (e.g., superficial wound after a fall, otitis externa following swimming in a pool). Two patients in the NYDA group experienced ocular irritation after treatment when the product entered the eyes. The irritation resolved spontaneously in both cases after rinsing the eyes with clean water .

Precaution

Use with caution in patients with autonomic neuropathy, hepatic or renal disease, ulcerative colitis, coronary heart disease, congestive heart failure, cardiac tachyarrhythmia, known or suspected prostatic hypertrophy.

Interaction

The following agents may increase certain actions or side-effects of Dicycloverine-antiarrhythmic agents, antihistamines, antipsychotic agents, benzodiazepines, MAO inhibitors, narcotic analgesics, nitrates and nitrites, sympathomimetic agents, tricyclic antidepressants and other drugs having anticholinergic activity.

Volume of Distribution

The volume of distribution for a 20mg oral dose is 3.65L/kg.

Following injection of [14C]dimethicone fluid in the hind limb of rats, the radioactivity was distributed primarily in the gastrointestinal tract, and no evidence of metabolism was observed. When [14C]dimethicone was administered through i.p. injection in rats, the following distribution of radioactivity was observed at 25 days after dosing: 51% in adipose tissue, 27% in gastrointestinal tissues, and 15% in liver .

Elimination Route

The bioavailability of dicyclomine has not been determined, though it is likely well absorbed as the primary route of elimination is in the urine. Dicyclomine has a T_max of 1-1.5h.

This drug is not believed to be absorbed when used in quantities from 1-30% .

Half Life

The mean plasma elimination half life is approximately 1.8 hours.

Clearance

Data regarding the clearance of dicyclomine is not readily available.

Elimination Route

Dicyclomine is 79.5% eliminated in the urine and 8.4% in the feces.

Pregnancy & Breastfeeding use

Pregnancy: Category B. Dicycloverine was neither teratogenic nor embryocidal in animal trial. It, like other drugs should be used during pregnancy only if clearly needed. There are no data on the secretion of this drug into breast milk. Dicycloverine should be used cautiously in case of lactating mother.

Contraindication

Dicycloverine is contraindicated in:

• Obstructive uropathy
• Obstructive disease of the gastrointestinal tract
• Severe ulcerative colitis
• Reflux esophagitis
• Unstable cardiovascular status in acute hemorrhage
• Glaucoma
• Myasthenia gravis
• Evidence of prior hypersensitivity to dicycloverine hydrochloride or other ingredients of this formulation
• Infants less than 6 months of age

Acute Overdose

Toxic reaction seldom occurs with dicycloverine. The signs and symptoms of overdosage are headache; nausea; vomiting; blurred vision; dilated pupils; hot, dry skin; dizziness; dryness of the mouth; difficulty in swallowing; and CNS stimulation.

Storage Condition

Store below 30°C.

Innovators Monograph

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