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DRUGS & SUPPLEMENTS
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Dicyclomine:
Actispas-R (Dicyclomine) hydrochloride is an antispasmodic and anticholinergic (antimuscarinic) agent. Actispas-R (Dicyclomine) hydrochloride occurs as a fine, white, crystalline, practically odorless powder with a bitter taste. It is soluble in water, freely soluble in alcohol and chloroform, and very slightly soluble in ether.
Chemically, it is [Bicyclohexyl]-1-carboxylic acid, 2-(diethyl-amino) ethyl ester, hydrochloride with the following structural formula:
C19H35NO2-HCI 345.95
Each capsule, for oral administration, contains 10 mg of Actispas-R (Dicyclomine) hydrochloride.
Each tablet, for oral administration, contains 20 mg of Actispas-R (Dicyclomine) hydrochloride.
This product contains the following inactive ingredients: colloidal silicon dioxide (tablets only), corn starch (tablets only), D&C red #28 (capsules only), FD&C blue #1 (capsules only), FD&C blue #1 lake (tablets only), FD&C red #40 (capsules only), gelatin (capsules only), hypromellose (tablets only), lactose monohydrate (tablets only), magnesium stearate (capsules only), pregelatinized starch, silicon dioxide (capsules only), sodium lauryl sulfate (capsules only), sodium starch glycolate (tablets only), and stearic acid (tablets only).
Actispas-R (Dicyclomine) Hydrochloride Structural Formula
Actispas-R (Dicyclomine) relieves smooth muscle spasm of the gastrointestinal tract. Animal studies indicate that this action is achieved via a dual mechanism: (1) a specific anticholinergic effect (antimuscarinic) at the acetylcholine- receptor sites with approximately 1/8 the milligram potency of atropine (in vitro, guinea pig ileum); and (2) a direct effect upon smooth muscle (musculotropic) as evidenced by dicyclomine's antagonism of bradykinin- and histamine-induced spasms of the isolated guinea pig ileum. Atropine did not affect responses to these two agonists. In vivo studies in cats and dogs showed Actispas-R (Dicyclomine) to be equally potent against acetylcholine (ACh)- or barium chloride (BaCI2)- induced intestinal spasm while atropine was at least 200 times more potent against effects of ACh than BaCI2. Tests for mydriatic effects in mice showed that Actispas-R (Dicyclomine) was approximately 1/500 as potent as atropine; antisialogogue tests in rabbits showed Actispas-R (Dicyclomine) to be 1/300 as potent as atropine.
In man, Actispas-R (Dicyclomine) is rapidly absorbed after oral administration, reaching peak values within 60-90 minutes. The principal route of elimination is via the urine (79.5% of the dose). Excretion also occurs in the feces, but to a lesser extent (8.4%). Mean half-life of plasma elimination in one study was determined to be approximately 1.8 hours when plasma concentrations were measured for 9 hours after a single dose. In subsequent studies, plasma concentrations were followed for up to 24 hours after a single dose, showing a secondary phase of elimination with a somewhat longer half-life. Mean volume of distribution for a 20 mg oral dose is approximately 3.65 L/kg suggesting extensive distribution in tissues.
In controlled clinical trials involving over 100 patients who received drug, 82% of patients treated for functional bowel/irritable bowel syndrome with Actispas-R (Dicyclomine) hydrochloride at initial doses of 160 mg daily (40 mg q.i.d.) demonstrated a favorable clinical response compared with 55% treated with placebo (p<.05). In these trials, most of the side effects were typically anticholinergic in nature and were reported by 61% of the patients.
Actispas-R (Dicyclomine) | ||
Hydrochloride | ||
(40 mg q.i.d.) | Placebo | |
Side Effect | % | % |
Dry Mouth | 33 | 5 |
Dizziness | 29 | 2 |
Blurred Vision | 27 | 2 |
Nausea | 14 | 6 |
Light-headedness | 11 | 3 |
Drowsiness | 9 | 1 |
Weakness | 7 | 1 |
Nervousness | 6 | 2 |
Nine percent (9%) of patients were discontinued from the drug because of one or more of these side effects (compared with 2% in the placebo group). In 41% of the patients with side effects, side effects disappeared or were tolerated at the 160 mg daily dose without reduction. A dose reduction from 160 mg daily to an average daily dose of 90 mg was required in 46% of the patients with side effects who then continued to experience a favorable clinical response; their side effects either disappeared or were tolerated.
For the treatment of functional bowel/irritable bowel syndrome.
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 Actispas-R (Dicyclomine) hydrochloride or other ingredients of these formulations
Infants less than 6 months of age
Nursing Mothers.
In the presence of a high environmental temperature, heat prostration can occur with drug use (fever and heat stroke due to decreased sweating). If symptoms occur, the drug should be discontinued and supportive measures instituted.
Diarrhea may be an early symptom of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy. In this instance, treatment with this drug would be inappropriate and possibly harmful.
Actispas-R (Dicyclomine) may produce drowsiness or blurred vision. The patient should be warned not to engage in activities requiring mental alertness, such as operating a motor vehicle or other machinery or performing hazardous work while taking this drug.
Psychosis has been reported in sensitive individuals given anticholinergic drugs. CNS signs and symptoms include confusion, disorientation, short-term memory loss, hallucinations, dysarthria, ataxia, coma, euphoria, decreased anxiety, fatigue, insomnia, agitation and mannerisms, and inappropriate affect. These CNS signs and symptoms usually resolve within 12 to 24 hours after discontinuation of the drug.
There are reports that administration of Actispas-R (Dicyclomine) syrup to infants has been followed by serious respiratory symptoms (dyspnea, shortness of breath, breathlessness, respiratory collapse, apnea, asphyxia), seizures, syncope, pulse rate fluctuations, muscular hypotonia, and coma. Death has been reported. No causal relationship between these effects observed in infants and Actispas-R (Dicyclomine) administration has been established. Actispas-R (Dicyclomine) IS CONTRAINDICATED IN INFANTS LESS THAN 6 MONTHS OF AGE AND IN NURSING MOTHERS..
Safety and efficacy of Actispas-R (Dicyclomine) hydrochloride in pediatric patients have not been established.
Use with caution in patients with:
Autonomic neuropathy
Hepatic or renal disease
Ulcerative colitis-large doses may suppress intestinal motility to the point of producing a paralytic ileus and the use of this drug may precipitate or aggravate the serious complication of toxic megacolon
Hyperthyroidism
Hypertension
Coronary heart disease
Congestive heart failure
Cardiac tachyarrhythmia
Hiatal hernia
Known or suspected prostatic hypertrophy.
Investigate any tachycardia before administration of Actispas-R (Dicyclomine) hydrochloride, since it may increase the heart rate.
With overdosage, a curare-like action may occur (i.e., neuromuscular blockade leading to muscular weakness and possible paralysis).
Actispas-R (Dicyclomine) may produce drowsiness or blurred vision. The patient should be warned not to engage in activities requiring mental alertness, such as operating a motor vehicle or other machinery or to perform hazardous work while taking this drug.
Actispas-R (Dicyclomine) is contraindicated in infants less than 6 months of age and in nursing mothers..
In the presence of a high environmental temperature, heat prostration can occur with drug use (fever and heat stroke due to decreased sweating).
If symptoms occur, the drug should be discontinued and a physician contacted.
The following agents may increase certain actions or side effects of anticholinergic drugs: amantadine, antiarrhythmic agents of Class I, antihistamines, antipsychotic agents (e.g., phenothiazines), benzodiazepines, MAO inhibitors, narcotic analgesics (e.g., meperidine), nitrates and nitrites, sympathomimetic agents, tricyclic antidepressants, and other drugs having anticholinergic activity.
Anticholinergics antagonize the effects of antiglaucoma agents. Anticholinergic drugs in the presence of increased intraocular pressure may be hazardous when taken concurrently with agents such as corticosteroids.
Anticholinergic agents may affect gastrointestinal absorption of various drugs, such as slowly dissolving dosage forms of digoxin; increased serum digoxin concentrations may result. Anticholinergic drugs may antagonize the effects of the drugs that alter gastrointestinal motility, such as metoclopramide. Because antacids may interfere with the absorption of anticholinergic agents, simultaneous use of these drugs should be avoided.
The inhibiting effects of anticholinergic drugs on gastric hydrochloric acid secretion are antagonized by agents used to treat achlorhydria and those used to test gastric secretion.
There are no known human data on long-term potential for carcinogenicity or mutagenicity.
Long-term studies in animals to determine carcinogenic potential are not known to have been conducted.
In studies in rats at doses of up to 100 mg/kg/day, Actispas-R (Dicyclomine) produced no deleterious effects on breeding, conception, or parturition.
Pregnancy Category B.
Reproduction studies have been performed in rats and rabbits at doses up to 33 times the maximum recommended human dose based on 160 mg/day and have revealed no evidence of impaired fertility or harm to the fetus due to Actispas-R (Dicyclomine). Epidemiologic studies in pregnant women with products containing Actispas-R (Dicyclomine) hydrochloride (at doses up to 40 mg/day) have not shown that Actispas-R (Dicyclomine) increases the risk of fetal abnormalities if administered during the first trimester of pregnancy. There are, however, no adequate and well-controlled studies in pregnant women at the recommended doses (80-160 mg/day). Because animal reproduction studies are not always predictive of human response, Actispas-R (Dicyclomine) as indicated for functional bowel/irritable bowel syndrome should be used during pregnancy only if clearly needed.
Since Actispas-R (Dicyclomine) has been reported to be excreted in human milk, Actispas-R (Dicyclomine) HYDROCHLORIDE IS CONTRAINDICATED IN NURSING MOTHERS..
Actispas-R (Dicyclomine) IS CONTRAINDICATED IN INFANTS LESS THAN 6 MONTHS OF AGE.
Safety and effectiveness in pediatric patients have not been established.
Controlled clinical trials have provided frequency information for reported adverse effects of Actispas-R (Dicyclomine) hydrochloride listed in a decreasing order of frequency.
Not all of the following adverse reactions have been reported with Actispas-R (Dicyclomine) hydrochloride. Adverse reactions are included here that have been reported for pharmacologically similar drugs with anticholinergic/antispasmodic action.
Gastrointestinal: dry mouth, nausea, vomiting, constipation, bloated feeling, abdominal pain, taste loss, anorexia
Central Nervous System: dizziness, light-headedness, tingling, headache, drowsiness, weakness, nervousness, numbness, mental confusion and/or excitement (especially in elderly persons), dyskinesia, lethargy, syncope, speech disturbance, insomnia
Ophthalmologic: blurred vision, diplopia, mydriasis, cycloplegia, increased ocular tension
Dermatological/Allergic: rash, urticaria, itching, and other dermal manifestations; severe allergic reaction or drug idiosyncrasies including anaphylaxis
Genitourinary: urinary hesitancy, urinary retention
Cardiovascular: tachycardia, palpitations
Respiratory: Dyspnea, apnea, asphyxia
Other: decreased sweating, nasal stuffiness or congestion, sneezing, throat congestion, impotence, suppression of lactation
Abuse of and/or dependence on Actispas-R (Dicyclomine) for anticholinergic effects have been rarely reported.
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. A curare-like action may occur.
A 37-year-old female reported numbness on the left side, cold fingertips, blurred vision, abdominal and flank pain, decreased appetite, dry mouth, and nervousness following ingestion of 320 mg daily (four 20 mg tablets QID) for four days. These events resolved after discontinuing the Actispas-R (Dicyclomine).
The acute oral LD50 of the drug is 625 mg/kg in mice.
Minimum Human Lethal Dose/Maximum Human Dose Recorded
The amount of drug in a single dose that is ordinarily associated with symptoms of overdosage or that is Iikely to be life threatening, has not been defined. The maximum human oral dose recorded was 600 mg by mouth in a 10-month-old child and approximately 1500 mg in an adult, each of whom survived.
In three of the infants who died following administration of Actispas-R (Dicyclomine) hydrochloride, the blood concentrations of drug were 200, 220, and 505 ng/mL, respectively.
It is not known if Actispas-R is dialyzable.
Treatment should consist of gastric lavage, emetics, and activated charcoal. Sedatives (e.g., short-acting barbiturates, benzodiazepines) may be used for management of overt signs of excitement. If indicated, an appropriate parenteral cholinergic agent may be used as an antidote.
DOSAGE MUST BE ADJUSTED TO INDIVIDUAL PATIENT NEEDS.
The only oral dose clearly shown to be effective is 160 mg per day (in 4 equally divided doses). Since this dose is associated with a significant incidence of side effects, it is prudent to begin with 80 mg per day (in 4 equally divided doses). Depending upon the patient's response during the first week of therapy, the dose should be increased to 160 mg per day unless side effects limit dosage escalation.
If efficacy is not achieved within 2 weeks or side effects require doses below 80 mg per day, the drug should be discontinued. Documented safety data are not available for doses above 80 mg daily for periods longer than 2 weeks.
The intramuscular dosage form is to be used temporarily when the patient cannot take oral medication. Intramuscular injection is about twice as bioavailable as oral dosage forms; consequently, the recommended intramuscular dose is 80 mg daily (in 4 equally divided doses).
Oral Actispas-R (Dicyclomine) hydrochloride should be started as soon as possible and the intramuscular form should not be used for periods longer than 1 or 2 days.
Actispas-R Hydrochloride Capsules USP and Actispas-R (Dicyclomine) Hydrochloride Tablets USP are supplied as follows:
10 mg capsules: Clear Dark Blue cap/Clear Dark Blue body hard gelatin capsules, imprinted with white ink WATSON over 794 on cap and 10 mg on the body, in bottles of 100 and 1000.
20 mg tablets: Blue, round, unscored, flat-faced, beveled-edge tablets, debossed WATSON and 795 on the periphery on one side and plain on the other side, in bottles of 100 and 1000.
Store at controlled room temperature 15°-30°C (59°-86°F).
Dispense in a well-closed container as defined in USP/NF.
Manufactured for:
Watson Laboratories, Inc.
Corona, CA 92880 USA
Manufactured by:
Patheon Pharmaceuticals Inc.
Cincinnati, OH 45215 USA
Ranitidine:
Actispas-R is a blocker of histamine H2-receptors. Inhibits basal and stimulated by histamine, gastrin and acetylcholine (to a lesser extent) the secretion of hydrochloric acid. Increases the pH of gastric contents and reduces the activity of pepsin. The duration of action of Actispas-R (Ranitidine) with a single admission - 12 hours.
After oral administration, Actispas-R (Ranitidine) is rapidly absorbed from the gastrointestinal tract. Eating and antacids significantly affect the extent of absorption. Subjected to the effect of "first passage" through the liver. Cmax in plasma is reached within 2 h after a single oral administration. After IM injection Actispas-R (Ranitidine) rapidly and almost completely absorbed from the injection site. Cmax achieved within 15 min.
Protein binding - 15%. Vd - 1.4 L / kg. Actispas-R (Ranitidine) is excreted in breast milk.
T1/2 is 2-3 h. About 30% of the dose excreted in the urine in unchanged form. Elimination rate decreases with abnormal liver function or renal function.
Gastric ulcer and duodenal ulcer in acute phase; prevention of relapse of peptic ulcer; symptomatic ulcer; erosive and reflux esophagitis; Zollinger-Ellison syndrome; prevention of "stress" ulcers of the gastrointestinal tract, postoperative ulcers, recurrent bleeding from upper gastrointestinal tract; prevention of aspiration of gastric juice during operations under general anesthesia.
Individual. For oral administration for treatment of adults and children over 14 years daily Actispas-R dose is 300-450 mg; if necessary, the daily dose was increased to 600-900 mg; multiplicity of administration is 2-3 times / day. For the prevention of exacerbations of disease are used by 150 mg / day at bedtime. The duration of treatment is determined by the indications for use.
The dose of Actispas-R (Ranitidine) for patients with renal insufficiency at the level of creatinine more than 3.3 mg / 100 ml is 75 mg 2 times / day.
IV or IM by 50-100 mg every 6-8 hours.
Cardio-vascular system: in a few cases (for IV administration) - AV-blockade.
Digestive system: rarely - diarrhea, constipation, and in isolated cases - hepatitis.
CNS: Rarely - headache, dizziness, fatigue, blurred vision, and in isolated cases (at seriously ill patients) - confusion, hallucinations.
Hematopoietic system: rarely - thrombocytopenia, prolonged use at high doses - leukopenia.
Metabolism: rarely - a slight increase of creatinine in serum at the beginning of treatment.
Endocrine system: long-term use in high doses may increase the content of prolactin, gynecomastia, amenorrhea, impotence, decreased libido.
From the musculoskeletal system: very rarely - arthralgia, myalgia.
Allergic reactions: rarely - a skin rash, urticaria, angioedema, anaphylactic shock, bronchospasm, hypotension.
Other: rarely - recurrent parotitis, and in isolated cases - hair loss.
Pregnancy, lactation (breastfeeding), increased sensitivity to Actispas-R (Ranitidine).
Adequate and well controlled studies of the safety of Actispas-R during pregnancy has not been conducted, therefore the use during pregnancy is contraindicated.
If necessary the use of Actispas-R (Ranitidine) during lactation should stop breastfeeding.
With careful use in patients with impaired renal excretory function.
Before treatment with Actispas-R (Ranitidine) is necessary to exclude the possibility of a malignant disease of the esophagus, stomach or duodenum.
With long-term treatment of debilitated patients under stress conditions may be bacterial lesions of the stomach with subsequent spread of infection.
Undesirable abrupt discontinuation of Actispas-R (Ranitidine) because of the risk of recurrence of peptic ulcer. Effectiveness of prophylactic treatment of peptic ulcer above while taking Actispas-R (Ranitidine) courses for 45 days in spring and autumn than during the reception. Quick intravenous injection of Actispas-R (Ranitidine) in rare cases cause bradycardia, usually in patients predisposed to cardiac arrhythmias.
There are a few reports that Actispas-R (Ranitidine) might contribute to the development of acute attacks of porphyria, in connection with what is necessary to avoid its use in patients with acute porphyria in history.
Therapy with Actispas-R (Ranitidine) possible distortions of laboratory data: increased creatinine, the activity of gamma-glutamyl transpeptidase and liver transaminases in the blood plasma.
In cases where Actispas-R (Ranitidine) is used in combination with antacids, the break between taking antacids and Actispas-R (Ranitidine) should be at least 1-2 hours (antacids may cause undesired absorption of Actispas-R (Ranitidine)).
Clinical data on the safety of Actispas-R (Ranitidine) in pediatric patients is limited.
In an application with antacids may decrease absorption of Actispas-R (Ranitidine).
In an application of Actispas-R (Ranitidine) with anticholinergics may be in breach of memory and attention in elderly patients.
Probably that histamine H2-blockers reduce receptor ulcerogenic action of NSAIDs on the gastric mucosa.
In an application with warfarin may decrease clearance of warfarin. There is one case of gipoprotrombinemiey and bleeding in patients receiving warfarin.
In an application with bismuth tripotassium dicitrate may increase unwanted absorption of bismuth, with glyburide - described the cases of hypoglycemia, with ketoconazole, itraconazole - decreased absorption of ketoconazole, itraconazole.
In an application with metoprolol may increase the plasma concentrations and increased AUC and T1 / 2 of metoprolol.
In an application with sucralfate in high doses (2 g) possible violation of the absorption of Actispas-R (Ranitidine).
In an application Actispas-R (Ranitidine) with procainamide may be decrease excretion of procainamide by the kidneys which leads to an increase in its concentration in blood plasma.
There is a data of increased absorption of triazolam in its simultaneous application, apparently due to changes in pH of gastric contents under the influence of Actispas-R (Ranitidine).
Probably that while the application with phenytoin may increase the concentration of phenytoin in plasma and increased risk of toxicity.
In an application with furosemide moderately expressed increasing the bioavailability of furosemide.
There is a described case of ventricular arrhythmias (bigeminy) with simultaneous application of quinidine, with cisapride - described a case of cardiotoxicity.
It can not be excluded some increase in cyclosporine concentration in blood plasma in its simultaneous application with Actispas-R (Ranitidine).
Symptoms: seizures, bradycardia, ventricular arrhythmias.
Treatment: induction of vomiting or gastric lavage, symptomatic therapy. In convulsions - diazepam IV, bradycardia - atropine, ventricular arrhythmias - lidocaine.
Depending on the reaction of the Actispas-R after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Actispas-R not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.
Is Actispas-R addictive or habit forming?Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.
Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.
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The information was verified by Dr. Rachana Salvi, MD Pharmacology