Symptoms and Signs
Aciloc is very specific in action and no particular problems are expected following overdosage with Aciloc formulations.
Treatment
Symptomatic and supportive therapy should be given as appropriate.
Symptoms and Signs
Ranitidine is very specific in action and no particular problems are expected following overdose with the drug. Up to 6g per day has been administered without untoward effect.
Treatment
Symptomatic and supportive therapy should be given as appropriate. If need be, the drug may be removed from the plasma by haemodialysis.
Aciloc products are contraindicated in patients known to have hypersensitivity to any component of the preparation.
Ranitidine is contraindicated for people known to be hypersensitive to the drug or any of the ingredients of Aciloc 75 Relief tablets.
Not applicable
None known
The following convention has been utilised for the classification of undesirable effects: Very common (> 1/10), Common > 1/100 to < 1/10), Uncommon >1/1,000 to < 1/100) Rare (> 1/10,000 to < 1/1,000), Very rare (< 1/10,000), not known (frequency cannot be estimated from the available data).
Adverse event frequencies have been estimated from spontaneous reports from post-marketing data.
Blood & Lymphatic System Disorders
Very Rare: Blood count changes (leucopenia, thrombocytopenia). These are usually reversible. Agranulocytosis or pancytopenia, sometimes with marrow hypoplasia or marrow aplasia.
Immune System Disorders
Rare: Hypersensitivity reactions (urticaria, angioneurotic oedema, fever, bronchospasm, hypotension and chest pain).
Very Rare: Anaphylactic shock
Unknown: dyspnoea
These events have been reported after a single dose.
Psychiatric Disorders
Very Rare: Reversible mental confusion, depression and hallucinations.
These have been reported predominantly in severely ill patients, in elderly and in nephropatic patients.
Nervous System Disorders
Very Rare: Headache (sometimes severe), dizziness and reversible involuntary movement disorders.
Eye Disorders
Very Rare: Reversible blurred vision.
There have been reports of blurred vision, which is suggestive of a change in accommodation.
Cardiac Disorders
Very Rare: As with other H2 receptor antagonists bradycardia, A-V block and tachycardia (for all formulations).
Vascular Disorders
Very Rare: Vasculitis.
Gastrointestinal Disorders
Very Rare: Acute pancreatitis, diarrhoea
Uncommon: abdominal pain, , constipation, nausea (these symptoms mostly improved during continued treatment).
Hepatobiliary Disorders
Rare: Transient and reversible changes in liver function tests.
Very Rare: Hepatitis (hepatocellular, hepatocanalicular or mixed) with or without jaundice, these were usually reversible.
Skin and Subcutaneous Tissue Disorders
Rare: Skin rash.
Very Rare: Erythema multiforme, alopecia.
Musculoskeletal and Connective Tissue Disorders
Very Rare: Musculoskeletal symptoms such as arthralgia and myalgia.
Renal and Urinary Disorders
Very rare: Acute interstitial nephritis.
Rare: elevation of plasma creatinine (usually slight; normalised during continued treatment)
Reproductive System and Breast Disorders
Very Rare: Reversible impotence, breast symptoms and breast conditions (such as gynaecomastia and galactorrhoea)
Paediatric population:
The safety of Aciloc has been established in children aged 0-16 years with gastric acid-related disease and was generally well tolerated with an adverse event profile resembling that in adults. There are limited safety data available on long-term use, in particular in relation to growth and development.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via
Yellow Card Scheme.
Website: www.mhra.gov.uk/yellowcard.
The following convention has been utilised for the >
Blood & Lymphatic System Disorders
Very Rare:
Blood count changes (leucopenia, thrombocytopenia). These are usually reversible. Agranulocytosis or pancytopenia, sometimes with marrow hypoplasia or marrow aplasia.
Immune System Disorders
Rare:
Hypersensitivity reactions (urticaria, angioneurotic oedema, fever, bronchospasm, hypotension and chest pain).
Very Rare:
Anaphylactic shock
These events have been reported after a single dose.
Psychiatric Disorders
Very Rare:
Reversible mental confusion, depression and hallucinations.
These have been reported predominantly in severely ill and elderly patients.
Nervous System Disorders
Very Rare:
Headache (sometimes severe),dizziness and reversible involuntary movement disorders.
Eye Disorders
Very Rare:
Reversible blurred vision.
There have been reports of blurred vision, which is suggestive of a change in accommodation.
Cardiac Disorders
Very Rare:
As with other H2 receptor antagonists bradycardia and A-V Block.
Vascular Disorders
Very Rare:
Vasculitis.
Gastrointestinal Disorders
Very Rare:
Acute pancreatitis. Diarrhoea.
Uncommon:
Abdominal pain, constipation, nausea. (these symptoms mostly improved during continued treatment).
Hepatobiliary Disorders
Rare:
Transient and reversible changes in liver function tests.
Very Rare
Hepatitis (hepatocellular, hepatocanalicular or mixed) with or without jaundice, these were usually reversible.
Skin and Subcutaneous Tissue Disorders
Rare:
Skin Rash.
Very Rare:
Erythema multiforme, alopecia.
Musculoskeletal and Connective Tissue Disorders
Very Rare:
Musculoskeletal symptoms such as arthralgia and myalgia.
Renal and Urinary Disorders
Very rare:
Acute interstitial nephritis.
Rare:
Elevation of plasma creatinine (usually slight; normalised during continued treatment)
Reproductive System and Breast Disorders
Very Rare:
Reversible impotence. Breast symptoms and breast conditions (such as gynaecomastia and galactorrhea).
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.
No additional data of relevance.
Extensive studies have been carried out in animals. The pharmacology of ranitidine hydrochloride shows it to be a surmountable H2 receptor antagonist which produces an inhibition of gastro acid secretion. Extensive toxicological investigators have been conducted which predicted a very safe profile for clinical use. This safety has been confirmed by extensive use in patients for many years.
ATC Code: A02B A02 - Drugs for peptic ulcers and gastro-oesophageal reflux disease (GORD); H2-receptor antagonists
Aciloc is a specific, rapidly acting histamine H2-antagonist.
Aciloc inhibits basal and stimulated secretion of gastric acid, reducing both the volume and the acid and pepsin content of the secretion. Aciloc has a relatively long duration of action and so a single 150mg dose effectively suppresses gastric acid secretion for 12 hours.
ATC Code
Pharmacotherapeutic group: H2-receptor antagonist, ATC code: A02BA02
Pharmacotherapeutic group
H2-receptor antagonists, ATC code: A02BA02
Mechanism of Action
Ranitidine is a specific, rapidly acting histamine H2-antagonist. It inhibits basal and stimulated secretion of gastric acid, reducing both the volume and the acid and pepsin content of the secretion
Pharmacodynamic Effects
Ranitidine has a long duration of action and a single 75 mg dose effectively suppresses gastric acid secretion for at least 12 hours.
Absorption
Following oral administration of 150 mg Aciloc, maximum plasma concentrations (300 to 550 ng/mL) occurred after 1—3 hours. Two distinct peaks or plateau in the absorption phase result from reabsorption of drug excreted into the intestine. The absolute bioavailability of Aciloc is 50-60% and plasma concentrations increase proportionally with increasing dose up to 300 mg.
Distribution
Aciloc is not extensively bound to plasma proteins (15%), but exhibits a large volume of distribution ranging from 96 to 142 L.
Metabolism
Aciloc is not extensively metabolised. The fraction of the dose recovered as metabolites is similar after both oral and i.v. dosing; and includes 6% of the dose in urine as the N-oxide, 2% as the S-oxide, 2% as desmethylAciloc and 1 to 2% as the furoic acid analogue.
Elimination
Plasma concentrations decline bi-exponentially, with a terminal half-life of 2-3 hours. The major route of elimination is renal. After IV administration of 150 mg 3H-Aciloc, 98% of the dose was recovered, including 5% in faeces and 93% in urine, of which 70% was unchanged parent drug. After oral administration of 150 mg 3H-Aciloc, 96% of the dose was recovered, 26% in faeces and 70% in urine of which 35% was unchanged parent drug. Less than 3% of the dose is excreted in bile. Renal clearance is approximately 500 mL/min, which exceeds glomerular filtration indicating net renal tubular secretion.
Special Patient Populations
Children (3 years and above)
Limited pharmacokinetic data have shown that there are no significant differences in half-life (range for children 3 years and above: 1.7 - 2.2 h) and plasma clearance (range for children 3 years and above: 9 - 22ml/min/kg) between children and healthy adults receiving oral Aciloc when correction is made for body weight.
Patients over 50 years of age
In patients over 50 years of age, half-life is prolonged (3-4 h) and clearance is reduced, consistent with the age-related decline of renal function. However, systemic exposure and accumulation are 50% higher. This difference exceeds the effect of declining renal function, and indicates increased bioavailability in older patients.
Absorption
Following oral administration of 150 mg ranitidine, maximum plasma concentrations (300 to 550 ng/mL) occurred after 1-3 hours. Two distinct peaks or a plateau in the absorption phase result from reabsorption of drug excreted into the intestine. The absolute bioavailability of ranitidine is 50-60%, and plasma concentrations increase proportionally with increasing dose up to 300 mg.
Absorption is not significantly impaired by food or antacids.
Distribution
Ranitidine is not extensively bound to plasma proteins (15%), but exhibits a large volume of distribution ranging from 96 to 142 L.
Metabolism
Ranitidine is not extensively metabolised. The fraction of the dose recovered as metabolites includes 6% of the dose in urine as the N-Oxide, 2% as the S-Oxide, 2% as desmethyl ranitidine and 1-2% as the furoic acid analogue.
Elimination
Plasma concentrations decline bi-exponentially, with a terminal half-life of 2-3 hours. The major route of elimination is renal. After IV administration of 150 mg 3H- ranitidine, 98% of the dose was recovered, including 5% in the faeces and 93% in the urine, of which 70% was unchanged parent drug. After oral administration of 150 mg 3H-ranitidine, 96% of the dose was recovered, 26% in the faeces and 70% in urine of which 35% was unchanged parent drug. Less than 3% of the dose is excreted in bile. Renal clearance is approximately 500mL/min, which exceeds glomerular filtration indicating net renal tubular secretion.
Special Patient Populations
- Patients over 50 years of age
In patients over 50 years of age, half-life is prolonged (3-4 h) and clearance is reduced, consistent with the age-related decline of renal function. However, systemic exposure and accumulation are 50% higher. This difference exceeds the effect of declining renal function, and indicates increased bioavailability in older patients.
The possibility of malignancy should be excluded before commencement of therapy in patients with gastric ulcer [and if indications include dyspepsia; patients of middle age and over with new or recently changed dyspeptic symptoms must be included] as treatment with Aciloc may mask symptoms of gastric carcinoma.
Aciloc is excreted via the kidney and so plasma levels of the drug are increased in patients with renal impairment.
Rare clinical reports suggest that Aciloc may precipitate acute porphyric attacks. Aciloc should therefore be avoided in patients with a history of acute porphyria.
In patients such as the elderly, persons with chronic lung disease, diabetes or the immuno-compromised, there may be an increased risk of developing community acquired pneumonia.
A large epidemiological study showed an increased risk of developing community acquired pneumonia in current users of Aciloc alone versus those who had stopped treatment, with an observed adjusted relative risk increase of 1.82 (95% CI, 1.26-2.64). Post-marketing data indicate reversible mental confusion, depression, and hallucinations have been reported most frequently in severely ill and elderly patients.
Regular supervision of patients who are taking non-steroidal anti-inflammatory drugs concomitantly with Aciloc is recommended, especially in the elderly and in those with a history of peptic ulcer.
Treatment with a histamine H2-antagonist such as Aciloc 75 Relief may mask symptoms associated with carcinoma of the stomach and may therefore delay diagnosis of the condition.
Ranitidine is excreted via the kidney and so plasma levels of the drug are increased in patients with renal impairment (creatinine clearance less than 50 ml/min). Aciloc 75 Relief is not suitable for these patients without medical supervision.
People taking non-steroidal anti-inflammatory drugs, especially those with a history of peptic ulcer and the elderly, should not self-medicate with Aciloc 75 Relief but seek their doctor's advice before use.
People with a history of porphyria should avoid use of the product.
Consumers will be advised not to purchase a second pack of tablets without the advice of a pharmacist of doctor.
The product is not indicated in the following people without seeking their doctor's advice:
- Patients with renal impairment (creatinine clearance less than 50ml/min) and/or hepatic impairment.
- Patients under regular medical supervision for other reasons.
- Patients taking medications either physician prescribed or self-prescribed.
- Those with difficulty swallowing, persistent stomach pain or unintended weight loss in association with symptoms of indigestion.
- Those who are middle-aged or elderly with new or recently changed symptoms of indigestion.
In patients such as the elderly, persons with chronic lung disease, diabetes or the immunocompromised, there may be an increased risk of developing community acquired pneumonia.
A large epidemiological study showed an increased risk of developing community acquired pneumonia in current users of ranitidine alone versus those who had stopped treatment, with an observed adjusted relative risk increase of 1,82 (95% CI 1,26-2,64).
None reported.
No known effect
No special instructions
