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Pharmacokinetics of Ranitidine (zantac): RxList: "Oral Ranitidine HCl is 50% absorbed after oral administration, compared to an IV injection with mean peak levels of 440 to 545 ng/ml occurring at 2 to 3 hours after a 150-mg dose. The syrup, capsule, and effervescent formulations are bioequivalent to the tablets. In a pharmacodynamic comparison of the effervescent with the ranitidine HCl tablets, during the first hour after administration, the effervescent tablet formulation gave a significantly higher intragastric pH, by approximately 1 pH unit, compared to the ranitidine HCl tablets. The elimination half-life is 2.5 to 3 hours. Absorption is not significantly impaired by the administration of food or antacids. Propantheline slightly delays and increases peak blood levels of ranitidine HCl, probably by delaying gastric emptying and transit time. In one study, simultaneous administration of high-potency antacid (150 mmol) in fasting subjects has been reported to decrease the absorption of ranitidine HCl. Serum concentrations necessary to inhibit 50% of stimulated gastric acid secretion are estimated to be 36 to 94 ng/ml. Following a single oral dose of 150 mg, serum concentrations of ranitidine HCl are in this range up to 12 hours. However, blood levels bear no consistent relationship to dose or degree of acid inhibition. The principal route of excretion is the urine, with approximately 30% of the orally administered dose collected in the urine as unchanged drug in 24 hours. Renal clearance is about 410 ml per minute, indicating active tubular excretion. Four patients with clinically significant renal function impairment (creatinine clearance 25 to 35 ml per minute) administered 50 mg of ranitidine intravenously had an average plasma half-life of 4.8 hours, a ranitidine clearance of 29 ml per minute, and a volume of distribution of 1.76 l/kg. In general, these parameters appear to be altered in proportion to creatinine clearance."
http://www.rxlist.com/cgi/generic/ranit_cp.htm

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Ranitidine (Zantac) Use, precautions, side effects: "PROPER USE: May be taken with or without food. Since ranitidine is excreted by the kidney and metabolized by the liver, dosages of ranitidine need to be lowered in patients with significantly abnormal liver or kidney function. PRECAUTIONS: Antacids may decrease the absorption of ranitidine. Safety of ranitidine in children has not been established. Ranitidine is not habit forming. Ranitidine can interfere with the metabolism of alcohol. Patients taking ranitidine who drink alcohol may have elevated blood alcohol levels. SIDE EFFECTS: Minor side effects include constipation, diarrhea, fatigue, headache, insomnia, muscle pain, nausea, and vomiting. Major side effects are rare. They include agitation, anemia, confusion, depression, easy bruising or bleeding, hallucinations, hair loss, irregular heartbeat, rash, visual changes, and yellowing of the skin or eyes."
http://www.nwnet.co.uk/bullet/ranitidine.htm

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Ranitindine (Zantac) Mechanism of action and pharmacokinetics: Parkinsons information exchange: "Mechanism of Action: Ranitidine competitively inhibits the binding of histamine receptors on gastric parietal cells (designated as the HA receptor), thus reducing basal and nocturnal gastric acid secretion. The drug also decreases the amount of gastric acid released in response to stimuli such as food, caffeine, insulin, betazole, or pentagastrin. Ranitidine reduces the total volume of gastric juice, thereby indirectly decreasing pepsin secretion. The drug does not appear to alter gastric motility, gastric emptying, esophageal pressures, biliary secretions, or pancreatic secretions. Ranitidine is not an antimuscarinic anticholinergic. Ranitidine may aid in gastromucosal healing, and it may protect the mucosa from the irritant effects caused by aspirin and nonsteroidal antiinflammatory agents. Pharmacokinetics: The oral bioavailability of ranitidine is about 50-60% due to first-pass elimination. The presence of food in the GI tract does not appear to affect the extent or rate of absorption. The drug distributes throughout the body fluids and tissues, and can be found in breast milk and CSF. Using inhibition of pentagastrin-induced acid secretion as an indicator, ranitidine's effects persist for 8-12 hours. Ranitidine undergoes metabolism in the liver, and both the unchanged drug and its metabolites are excreted in the urine and feces. The half-life of the drug is 2-3 hours but increases to roughly 5 hours in anuric patients. Tubular secretion as well as glomerular filtration account for ranitidine renal elimination."
http://www.parkinsons-information-exchange-network-online.com/drugdb/113.html

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Ranitidine (zantac) interactions and precautions: GI care: "There are no known interactions with any food or alcohol. Alcohol and caffeine, which is found in coffee, tea, cola and chocolate, both stimulate stomach acid production and may worsen ulcer symptoms. Are there interactions with other drugs? An interaction generally means that one drug may increase or decrease the effect of another drug. Also, the more medications a person takes, the more likely there will be a drug interaction. Interactions with this drug may occur with the following: antacids blood thinners (Coumadin) diazepam (Valium) glipizide (Glucotrol) glyburide (Micronase, Diabeta) itraconazole (Sporanox) ketoconazole (Nizoral) metoprolol (Lopressor) nifedipine (Procardia) phenytoin (Dilantin) procainamide (Procanbid) sucralfate (Carafate) theophylline (Theo-Dur, Slo-bid) Ranitidine may cause drowsiness or dizziness. Do not drive or operate other hazardous machinery until the effect of the drug has been determined. Because smoking is a risk factor in peptic ulcer disease, stop smoking if possible. Taking ranitidine with antacids could prevent absorption of the ranitidine. If antacids are necessary while on ranitidine therapy, the doses should be staggered. Do not use over-the-counter doses for more than two weeks without physician approval."
http://www.gicare.com/pated/ranitidine.htm

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Ranitindine (Zantac) patient information: Focus on digestion: "PRESCRIBED FOR: Ranitidine blocks the action of histamine on stomach cells, and reduces stomach acid production. Ranitidine is useful in promoting healing of stomach and duodenal ulcers, and in reducing ulcer pain. Ranitidine has been effective in preventing ulcer recurrence when given in low doses for prolonged periods of time. In doses higher than that used in ulcer treatment, ranitidine has been helpful in treating heartburn and in healing ulcer and inflammation of the esophagus resulting from acid reflux (reflux esophagitis). DOSING: May be taken with or without food. Since ranitidine is excreted by the kidney and metabolized by the liver, dosages of ranitidine need to be lowered in patients with significantly abnormal liver or kidney function. DRUG INTERACTIONS: Antacids may decrease the absorption of ranitidine. Safety of ranitidine in children has not been established. Ranitidine is not habit forming. Ranitidine can interfere with the metabolism of alcohol. Patients taking ranitidine who drink alcohol may have elevated blood alcohol levels. SIDE EFFECTS: Minor side effects include constipation, diarrhea, fatigue, headache, insomnia, muscle pain, nausea, and vomiting. Major side effects are rare; they include: agitation, anemia, confusion, depression, easy bruising or bleeding, hallucinations, hair loss, irregular heartbeat, rash, visual changes, and yellowing of the skin or eyes."
http://www.focusondigestion.com/script/main/art.asp?articlekey=861&rd=1

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Can Ranitidine raise blood alcohol levels?: American Family Physician: "Previous studies of two histamine H2-receptor antagonists, cimetidine and ranitidine, suggest that they increase blood alcohol concentrations by decreasing the first pass metabolism of ethanol. Ranitidine has also been shown to accelerate gastric emptying of ethanol. While some studies have confirmed that ranitidine can increase blood alcohol levels, the effect was too small to be clinically significant. These studies did not include social drinkers, who tend to repetitively consume small amounts of ethanol. Arora and colleagues studied the impact of ranitidine on the blood alcohol levels of social drinkers. Men with a history of consuming fewer than five standard drinks per week were enrolled in the study. Social drinking was simulated with four small drinks, 150 mg per kg of ethanol, alternating with potato chips, given every 45 minutes. Breath analysis for ethanol was performed 15 minutes after the drink was consumed and then every five minutes until the next drink. After this initial test, the patients were given ranitidine in a dosage of 150 mg twice a day for one week. The consumption of small drinks and breath analysis were repeated. Blood alcohol levels rose after the patients took ranitidine for one week. In seven of the nine participants, blood alcohol levels while ranitidine was being taken exceeded 25 mg per dL (5.4 mmol per L), a level at which judgment and finely tuned skills are impaired. The high levels persisted for a longer time during ranitidine use than they had done before the medication was used."
http://www.findarticles.com/cf_dls/m3225/11_61/62829266/p1/article.jhtml

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Pharmacological action, pharmacokinetics and indications for Ranitidine (Zantac): inteKom: "PHARMACOLOGICAL ACTION: Ranitidine is a competitive H2-receptor antagonist and inhibits basal and stimulated secretions, acid and pepsin content, gastric mucous secretion is not affected. Ranitidine has no anti-serotinergic or antihistamine H1-receptor blocking activities, and it does not affect serum prolactin concentrations. It has no affinity for androgen, oestrogen, progesterone, or mineralocorticoid receptors. Pharmacokinetics: Peak plasma concentrations are usually reached within 2-3 hours following oral administration and the absorption is not influenced by food or antacids. With an elimination half-life of approximately 2-3 hours, ranitidine is excreted via kidneys in the free and metabolised forms. N-oxide is the main metabolite and S-oxide and desmethyl ranitidine in smaller quantities. There is normally no interaction between ranitidine and the cytochrome P450-linked drug metabolising enzyme system. Ranitidine crosses the placental barrier and is excreted into breast milk where concentrations are reported to be higher than in plasma. INDICATIONS: Ranitidine is indicated for the treatment of duodenal ulcers, benign gastric ulcer including prevention of duodenal ulceration associated with non-steroidal anti-inflammatory agents, reflux oesophagitis and the Zollinger-Ellison syndrome. To minimise the consequences of acids-aspiration syndrome during anaesthesia, ranitidine is used as premedication to reduce volume and acid content of gastric secretion. CONTRA-INDICATIONS: Any known hypersensitivity to any of the ingredients. Safety during pregnancy and lactation has not been established. Patients with a known history of porphyria should avoid taking APO-RANITIDINE"
http://home.intekom.com/pharm/apotex/a-ranit.html

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Before Using Ranitidine (Zantac): Medlineplus: "In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For ranitidine bismuth citrate, the following should be considered: Allergies--Tell your doctor if you have ever had any unusual or allergic reaction to ranitidine bismuth citrate. Also tell your health care professional if you are allergic to any other substances, such as foods, preservatives, or dyes. Pregnancy--Studies have not been done in pregnant women. A few women who became pregnant during studies of ranitidine bismuth citrate delivered normal infants; one woman with a history of problems during pregnancy delivered an infant with a birth defect. However, it is not known if this defect was caused by the medicine. Studies in pregnant animals have not shown that ranitidine bismuth citrate causes harmful effects in the offspring. Before taking this medicine, make sure your doctor knows if you are pregnant or if you may become pregnant. Breast-feeding--It is not known whether ranitidine bismuth citrate passes into breast milk. Although most medicines pass into breast milk in small amounts, many of them may be used safely while breast-feeding. Mothers who are taking this medicine and who wish to breast-feed should discuss this with their doctor. Children--Studies on this medicine have been done only in adult patients, and there is no specific information comparing use of ranitidine bismuth citrate in children with use in other age groups. Older adults--In studies done to date that have included older adults, ranitidine bismuth citrate has not been shown to cause different side effects or problems in older people than it does in younger adults. Other medicines--Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking ranitidine bismuth citrate, it is especially important that your health care professional know if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicines. Other medical problems--The presence of other medical problems may affect the use of ranitidine bismuth citrate. Make sure you tell your doctor if you have any other medical problems, especially: Acute porphyria, history of--Ranitidine bismuth citrate may make the condition worse Kidney disease--Higher blood levels of ranitidine bismuth citrate may result and increase the chance of side effects"
Office of Communications and Public Liaison National Library of Medicine
8600 Rockville Pike Bethesda, Maryland 20894
Phone: (301) 496-6308 Fax: (301) 496-4450 email: publicinfo@nlm.nih.gov
http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a601106.html

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