Diclogesic Spas

Acetaminophen:

• Pharmacological action
• Why is Diclogesic Spas (Acetaminophen) prescribed?
• Diclogesic Spas dosage and administration
• Diclogesic Spas side effects, adverse reactions
• Contraindications
• Using during pregnancy and breastfeeding
• Special Instructions
• Diclogesic Spas (Acetaminophen) Drug Interactions
• Diclogesic Spas in case of emergency / overdose
• Diclogesic Spas (Acetaminophen) reviews

Pharmacological action

Diclogesic Spas is an analgesic-antipyretic. It has analgesic, antipyretic and weak anti-inflammatory action. The mechanism of action is associated with inhibition of prostaglandin synthesis, the predominant influence on the thermoregulation center in the hypothalamus, enhances heat transfer.

Why is Diclogesic Spas (Acetaminophen) prescribed?

Pain weak and moderate intensity of different genesis (including headache, migraine, toothache, neuralgia, myalgia, algomenorrhea; pain in trauma, burns). Fever in infectious and inflammatory diseases.

Diclogesic Spas dosage and administration

Oral or rectally adults and adolescents with a body weight over 60 kg is used in a single dose of 500 mg, the multiplicity of admission - up to 4 times / Maximum duration of treatment - 5-7 days.

Maximum dose: single - 1 g, daily - 4 g.

Single dose for oral administration for children aged 6-12 years - 250-500 mg, 1-5 years - 120-250 mg, from 3 months to 1 year - 60-120 mg, up to 3 months - 10 mg / kg. Single dose rectal in children aged 6-12 years - 250-500 mg, 1-5 years - 125-250 mg.

Multiplicity - 4 at intervals of not less than 4 h. The maximum duration of treatment - 3 days.

Maximum dose: 4 single dose per day.

Diclogesic Spas side effects, adverse reactions

Digestive system: rarely - dyspepsia; long-term use at high doses - hepatotoxic effects, methemoglobinemia, renal dysfunction and liver, hypochromic anemia. Hemopoietic system: rarely - thrombocytopenia, leukopenia, pancytopenia, neutropenia, agranulocytosis. Allergic reactions: rarely - skin rash, itching, hives.

Contraindications

Chronic active alcoholism, increased sensitivity to Diclogesic Spas, marked disturbances of liver function and / or kidney disease, anemia, pregnancy (I term).

Using during pregnancy and breastfeeding

Diclogesic Spas (Acetaminophen) crosses the placental barrier. So far, no observed adverse effects of Diclogesic Spas (Acetaminophen) on the fetus in humans.

Diclogesic Spas (Acetaminophen) is excreted in breast milk: the content in milk was 0.04-0.23% of the dose adopted mother.

If necessary, use of Diclogesic Spas (Acetaminophen) during pregnancy and lactation (breastfeeding) should carefully weigh the potential benefits of therapy for the mother and the potential risk to the fetus or child.

In experimental studies found no embryotoxic, teratogenic and mutagenic action of Diclogesic Spas (Acetaminophen).

Special Instructions

Diclogesic Spas is used with caution in patients with disorders of the liver and kidneys, with benign hyperbilirubinemia, as well as in elderly patients.

With prolonged use of Diclogesic Spas (Acetaminophen) is necessary to monitor patterns of peripheral blood and functional state of the liver.

Used for treatment of premenstrual tension syndrome in combination with pamabrom (diuretic, a derivative of xanthine) and mepyramine (Histamine H1-receptors blocker).

Diclogesic Spas (Acetaminophen) Drug Interactions

With the simultaneous use with inducers of microsomal liver enzymes, means having hepatotoxic effect, increasing the risk of hepatotoxic action of Diclogesic Spas (Acetaminophen).

With the simultaneous use of anticoagulants may be slight to moderate increase in prothrombin time.

With the simultaneous use of anticholinergics may decrease absorption of Diclogesic Spas (Acetaminophen).

With the simultaneous use of oral contraceptives accelerated excretion of Diclogesic Spas (Acetaminophen) from the body and may reduce its analgesic action.

With the simultaneous use with urological means reduced their effectiveness.

With the simultaneous use of activated charcoal reduced bioavailability of Diclogesic Spas (Acetaminophen).

When Diclogesic Spas (Acetaminophen) applied simultaneously with diazepam may decrease excretion of diazepam.

There have been reports about the possibility of enhancing mielodepression effect of zidovudine while applying with Diclogesic Spas (Acetaminophen). A case of severe toxic liver injury.

Described cases of toxic effects of Diclogesic Spas (Acetaminophen), while the use of isoniazid.

When applied simultaneously with carbamazepine, phenytoin, phenobarbital, primidonom decreases the effectiveness of Diclogesic Spas (Acetaminophen), which is caused by an increase in its metabolism and excretion from the body. Cases of hepatotoxicity, while the use of Diclogesic Spas (Acetaminophen) and phenobarbital.

In applying cholestyramine a period of less than 1 h after administration of Diclogesic Spas (Acetaminophen) may decrease of its absorption.

At simultaneous application with lamotrigine moderately increased excretion of lamotrigine from the body.

With the simultaneous use of metoclopramide may increase absorption of Diclogesic Spas (Acetaminophen) and its increased concentration in blood plasma.

When applied simultaneously with probenecid may decrease clearance of Diclogesic Spas (Acetaminophen), with rifampicin, sulfinpyrazone - may increase clearance of Diclogesic Spas (Acetaminophen) due to increasing its metabolism in the liver.

At simultaneous application of Diclogesic Spas (Acetaminophen) with ethinylestradiol increases absorption of Diclogesic Spas (Acetaminophen) from the gut.

Enhances the effect of indirect anticoagulants (coumarin derivatives and indandione). Antipyretic and analgesic activity of caffeine increases, reduce - rifampicin, phenobarbital and alcohol (accelerated biotransformation, inducing microsomal liver enzymes).

Diclogesic Spas in case of emergency / overdose

At a reception in toxic doses (10-15 g in adults) may develop liver necrosis.

Symptoms of overdose may include: nausea, vomiting, loss of appetite, sweating, extreme tiredness, unusual bleeding or bruising, pain in the upper right part of the stomach, yellowing of the skin or eyes, flu-like symptoms

Diclofenac Sodium:

• Pharmacological action
• Pharmacokinetics
• Why is Diclogesic Spas prescribed?
• Dosage and administration
• Diclogesic Spas (Diclofenac Sodium) side effects
• Contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Diclogesic Spas (Diclofenac Sodium) drug interactions
• Diclogesic Spas in case of emergency / overdose
• Storage conditions
• Diclogesic Spas (Diclofenac Sodium) reviews

Pharmacological action

NSAIDs, a derivative of phenylacetic acid, Diclogesic Spas has a pronounced anti-inflammatory, analgesic and mild antipyretic effect. The mechanism of action is associated with inhibition of COX activity - the main enzyme metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. Analgesic effect is due to two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system).

Inhibits synthesis of proteoglycan in cartilage.

In rheumatic diseases, Diclogesic Spas (Diclofenac Sodium) reduces joint pain at rest and in motion, as well as morning stiffness and swelling of the joints, helps to increase range of motion; reduces post-traumatic and postoperative pain, and inflammatory edema.

Inhibits platelet aggregation. With prolonged use has a desensitizing effect.

When used topically in ophthalmology reduces swelling and pain in inflammatory processes non-infectious etiology.

Pharmacokinetics

After intake is absorbed from the gastrointestinal tract. Eating slows down the rate of absorption, extent of absorption is not changed. About 50% of the active substance is metabolized in the "first passage" through the liver. When used rectally absorption is slower. Time to reach C_max in plasma after oral administration is 2-4 hours depending on the used dosage form, after rectal - 1 h, I.M. administration - 20 min. The concentration of active substance in plasma is a linear function of the applied dose.

Not cumulative. Plasma protein binding is 99.7% (predominantly albumin). Penetrates into synovial fluid, C_max is achieved in 2-4 hours later than in plasma.

To a large extent metabolized to form several metabolites, among which two pharmacologically active, but to a lesser extent than Diclogesic Spas (Diclofenac Sodium).

Systemic clearance of the active substance is about 263 ml / min. T1/2 from plasma is 1-2 h, from synovial fluid - 3-6 h. Approximately 60% of the dose was excreted as metabolites by the kidneys, less than 1% excreted in the urine as unchanged, while the rest is displayed in the form of metabolites with bile.

Why is Diclogesic Spas prescribed?

Articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), degenerative and chronic inflammatory diseases of musculoskeletal system (osteochondrosis, osteoarthritis, periartropatii), post-traumatic inflammation of soft tissue and musculoskeletal system (sprains, bruises). Pain in the spine, neuralgia, myalgia, arthralgia, pain and inflammation after surgery or injury, pain in gout, migraine, algomenorrhea, pain with Bursitis, proctitis, colic (biliary and renal), pain in infectious and inflammatory diseases of ENT organs.

For local use: the inhibition of miosis during surgery for cataract prevention of cystoid macular edema associated with removal and lens implantation, inflammatory eye non-infectious nature, post-traumatic inflammation in penetrating and nonpenetrating wound of the eyeball.

Dosage and administration

For oral use for adult single dose is 25-50 mg 2-3 times / 24 h. Frequency of admission depends on the dosage form employed, the severity of the disease and is 1-3 times / 24 h, rectally - 1 times / 24 h, for the treatment of acute conditions or the exacerbation of chronic edema use intramuscular in dose of 75 mg.

For children older than 6 years and adolescents daily dose is 2 mg / kg.

Topical applied at a dose of 2-4 g on the affected area 3-4 times / 24 h.

When used in ophthalmology frequency and duration of administration are determined individually.

The maximum oral daily dose for adults is 150 mg.

Diclogesic Spas (Diclofenac Sodium) side effects

Digestive system: nausea, vomiting, anorexia, abdominal pain and discomfort in the epigastrium, flatulence, constipation, diarrhea, and in some cases - erosive-ulcerative lesions, gastrointestinal bleeding and perforation; rarely - abnormal liver function. When rectal administration - in isolated cases were observed inflammation of the colon bleeding, exacerbation of ulcerative colitis.

From the side of the central nervous system and peripheral nervous system: dizziness, headache, agitation, insomnia, irritability, fatigue, rarely - paresthesia, visual disturbances (blurred, double vision), tinnitus, insomnia, cramps, irritability, tremors, mental disorders, depression.

Hemopoietic system: rarely - anemia, leukopenia, thrombocytopenia, agranulocytosis.

Urinary system: rarely - renal failure; in predisposed patients may be swelling.

Dermatological reactions: rarely - hair loss.

Allergic reactions: skin rash, itching, when used in the form of eye drops - itching, redness, photosensitivity.

Local reactions: in the place of I.M. introducing possible burning, in some cases - the formation of infiltration, abscess, necrosis of adipose tissue in the rectal administration may be local irritation, the appearance of mucous discharge mixed with blood, painful defecation, when used externally, in rare cases - itching, redness, rash, burning sensation, when applied topically in ophthalmology may be a transient burning sensation and / or temporary blurred vision immediately after instillation.

With long-term topical use and / or drawing on a vast surface of body are possible systemic side effects due to resorptive action of Diclogesic Spas (Diclofenac Sodium).

Contraindications

known hypersensitivity to Diclogesic Spas sodium or to any accessory ingredient that is part of the drug Diclogesic Spas (Diclofenac Sodium);

anamnestic information about the attacks of bronchial asthma, urticaria, acute rhinitis associated with the use of aspirin or other NSAIDs;

hemodyscrasia unknown origin;

children under 6 years

pregnancy (III trimester);

lactation

increased sensitivity to sulfite (for injection solution).

children under age 15 - tablets of 50 mg to 18 years - injection.

Using during pregnancy and breastfeeding

Use during pregnancy and lactation is possible in cases where the potential benefits for the mother exceeds than the potential risk to the fetus or newborn.

Special instructions

With extreme caution is used in diseases of liver, kidney, gastrointestinal history, dyspepsia, asthma, hypertension, heart failure, after major surgery, as well as elderly patients.

When referring to a history of allergic reactions to NSAIDs Diclogesic Spas and sulfites are used only in urgent cases. In the course of treatment requires systematic monitoring of liver function and kidney picture of peripheral blood.

Do not recommended the use for rectal patients with diseases of anorectal region or anorectal bleeding in history. Topical should be applied only to intact skin areas.

Avoid contact with Diclogesic Spas (Diclofenac Sodium) in the eye (except for eye drops), or on mucous membranes. Patients who use contact lenses, eye drops should be applied no earlier than 5 minutes after removing the lenses.

Not recommended for children under 6 years.

During the period of treatment drugs for systemic use is not recommended alcohol consumption.

During the period of treatment may decrease the speed of psychomotor reactions. With worsening blurred vision after application of eye drops should not be driving and doing other potentially danger activities.

Diclogesic Spas (Diclofenac Sodium) drug interactions

At simultaneous application with Diclogesic Spas (Diclofenac Sodium) antihypertensive drugs may be weakening their actions.

There are few reports on the occurrence of seizures in patients taking both NSAIDs and antibacterial drugs quinolic series.

At simultaneous application with GCS and increased risk of side effects from the digestive system.

With simultaneous use of diuretics may decrease diuretic effect. With the simultaneous use of potassium-sparing diuretics may increase the concentration of potassium in the blood.

With simultaneous use with other NSAIDs may increase the risk of side effects.

There are reports of hypoglycemia or hyperglycemia in patients with diabetes who engaged in Diclogesic Spas (Diclofenac Sodium) together with hypoglycemic drugs.

When applied simultaneously with acetylsalicylic acid may decrease the concentration of Diclogesic Spas (Diclofenac Sodium) in plasma.

Although clinical studies have not found the influence of Diclogesic Spas (Diclofenac Sodium) on the action of anticoagulants, describes the individual cases of bleeding when used with Diclogesic Spas (Diclofenac Sodium) and warfarin.

With simultaneous use may increase digoxin, lithium, and phenytoin in blood plasma.

The absorption of Diclogesic Spas (Diclofenac Sodium) from the gastrointestinal tract is reduced by simultaneous application with kolestiraminom, to a lesser extent - with colestipol.

With simultaneous use may increase the concentration of methotrexate in plasma and increased its toxicity.

With simultaneous application of Diclogesic Spas (Diclofenac Sodium) could not affect the bioavailability of morphine, but the concentration of the active metabolite of morphine may be enhanced in the presence of Diclogesic Spas (Diclofenac Sodium), which increases the risk of side effects metabolites of morphine, including respiratory depression.

When applied simultaneously with pentazocine described a case of great convulsions, and rifampicin - may decrease the concentration of Diclogesic Spas (Diclofenac Sodium) in plasma, with ceftriaxone - increases excretion of ceftriaxone in bile; with cyclosporine - may increase cyclosporine nephrotoxicity.

Diclogesic Spas in case of emergency / overdose

Symptoms: may cause hypotension, renal failure, convulsions, gastrointestinal irritation or respiratory depression. Treatment: There is no specific antidote. In acute poisoning as soon as possible to stop drug absorption from the gastrointestinal tract. There is indicated gastric lavage, activated charcoal appointment and conduct of other symptomatic and supportive therapy. The use of forced diuresis, dialysis or blood transfusion is not justified because NSAIDs largely associated with serum proteins and possess extensive metabolism.

Storage conditions

In a dry, protected from light place, at temperature not above 25°C.Common expiration date for Diclogesic Spas (Diclofenac Sodium) tablets: 3 years.

Dicyclomine:

• Description
• Clinical pharmacology
• Indications and usage
• Contraindications
• Warnings
• Precautions
• Adverse reactions
• Drug abuse and dependence
• Overdosage
• Dosage and administration
• How supplied
• Diclogesic Spas (Dicyclomine) reviews

DESCRIPTION

Diclogesic Spas (Dicyclomine) hydrochloride is an antispasmodic and anticholinergic (antimuscarinic) agent. Diclogesic Spas (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 Diclogesic Spas (Dicyclomine) hydrochloride.

Each tablet, for oral administration, contains 20 mg of Diclogesic Spas (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).

Diclogesic Spas (Dicyclomine) Hydrochloride Structural Formula

CLINICAL PHARMACOLOGY

Diclogesic Spas (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 Diclogesic Spas (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 Diclogesic Spas (Dicyclomine) was approximately 1/500 as potent as atropine; antisialogogue tests in rabbits showed Diclogesic Spas (Dicyclomine) to be 1/300 as potent as atropine.

In man, Diclogesic Spas (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 Diclogesic Spas (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.

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.

INDICATIONS AND USAGE

For the treatment of functional bowel/irritable bowel syndrome.

CONTRAINDICATIONS

• 
  

  Obstructive uropathy
  

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  Obstructive disease of the gastrointestinal tract
  

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  Severe ulcerative colitis
  

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  Reflux esophagitis
  

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  Unstable cardiovascular status in acute hemorrhage
  

• 
  

  Glaucoma
  

• 
  

  Myasthenia gravis
  

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  Evidence of prior hypersensitivity to Diclogesic Spas (Dicyclomine) hydrochloride or other ingredients of these formulations
  

• 
  

  Infants less than 6 months of age
  

• 
  

  Nursing Mothers.
  

WARNINGS

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.

Diclogesic Spas (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 Diclogesic Spas (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 Diclogesic Spas (Dicyclomine) administration has been established. Diclogesic Spas (Dicyclomine) IS CONTRAINDICATED IN INFANTS LESS THAN 6 MONTHS OF AGE AND IN NURSING MOTHERS..

Safety and efficacy of Diclogesic Spas (Dicyclomine) hydrochloride in pediatric patients have not been established.

PRECAUTIONS

General

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 Diclogesic Spas (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).

Information For Patients

Diclogesic Spas (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.

Diclogesic Spas (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.

Drug Interactions

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.

Carcinogenesis, Mutagenesis, Impairment of Fertility

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, Diclogesic Spas (Dicyclomine) produced no deleterious effects on breeding, conception, or parturition.

Pregnancy

Teratogenic Effects

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 Diclogesic Spas (Dicyclomine). Epidemiologic studies in pregnant women with products containing Diclogesic Spas (Dicyclomine) hydrochloride (at doses up to 40 mg/day) have not shown that Diclogesic Spas (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, Diclogesic Spas (Dicyclomine) as indicated for functional bowel/irritable bowel syndrome should be used during pregnancy only if clearly needed.

Nursing Mothers

Since Diclogesic Spas (Dicyclomine) has been reported to be excreted in human milk, Diclogesic Spas (Dicyclomine) HYDROCHLORIDE IS CONTRAINDICATED IN NURSING MOTHERS..

Pediatric Use

Diclogesic Spas (Dicyclomine) IS CONTRAINDICATED IN INFANTS LESS THAN 6 MONTHS OF AGE.

Safety and effectiveness in pediatric patients have not been established.

ADVERSE REACTIONS

Controlled clinical trials have provided frequency information for reported adverse effects of Diclogesic Spas (Dicyclomine) hydrochloride listed in a decreasing order of frequency.

Not all of the following adverse reactions have been reported with Diclogesic Spas (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

DRUG ABUSE AND DEPENDENCE

Abuse of and/or dependence on Diclogesic Spas (Dicyclomine) for anticholinergic effects have been rarely reported.

OVERDOSAGE

Signs and Symptoms

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 Diclogesic Spas (Dicyclomine).

Oral LD₅₀

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 Diclogesic Spas (Dicyclomine) hydrochloride, the blood concentrations of drug were 200, 220, and 505 ng/mL, respectively.

Dialysis

It is not known if Diclogesic Spas is dialyzable.

Treatment

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 AND ADMINISTRATION

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 Diclogesic Spas (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.

HOW SUPPLIED

Diclogesic Spas Hydrochloride Capsules USP and Diclogesic Spas (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.

Storage

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