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Cimetidine capsules are a classic H2 receptor antagonist, with its core component being cimetdine. The chemical name is N '- methyl-N' '- [2 [[(5-methyl-1H-imidazol-4-yl) methyl] thio] ethyl] - N-cyanoguanidine, with a molecular formula of C10H16N6S and a molecular weight of 252.34. The drug is mainly in capsule form, with white or off white powder content, and the specification is usually 0.2 grams per capsule. Its chemical structure competitively binds to the H2 receptor on the basal membrane of gastric wall cells, blocking histamine induced gastric acid secretion and becoming one of the basic medicine for treating gastric acid related diseases.
Additional information of chemical compound:
Our product form
Cimetidine +. COA
Cimetidine capsules is a drug that inhibits gastric acid secretion, mainly used to treat diseases related to excessive gastric acid such as gastric ulcers, duodenal ulcers, reflux esophagitis, Zollinger Ellison syndrome, etc.
1. Gastric ulcer
Can be used to treat gastric ulcers. Gastric ulcer may be related to Helicobacter pylori infection, long-term use of nonsteroidal anti-inflammatory medicine, and other factors, usually manifested as upper abdominal pain, acid reflux, belching, and other symptoms. Patients can use dosis forms such as cimetdine tablets and capsules under the guidance of a doctor, combined with medicine such as amoxicillin capsules and clarithromycin tablets for combintion therapy.
2. Duodenal ulcer
Suitable for the tratment of duodenal ulcers. Duodenal ulcer is usually related to factors such as excessive gastric acid secretion and Helicobacter pylori infection. Common symptoms include hunger pain, nighttime pain, and black stool. Doctors may recommend the use of dosis forms such as cimetdine injection and granules, combined with medicine such as omeprazole enteric coated tablets and colloidal bismuth pectin capsules for comprehensive tratment.
3. Reflux esophagitis
Can alleviate the symptoms of reflux esophagitis. This disease may be related to factors such as dysfunction of the lower esophageal sphincter and increased gastric pressure, mainly manifested as symptoms such as burning sensation behind the sternum, acid reflux, and difficulty swallowing. Patients can use dosis forms such as cimetdine dispersible tablets under the guidance of a doctor, combined with medications such as domperidone tablets and magnesium aluminum carbonate chewable tablets to improve symptoms.
Pharmacokinetic characteristics
After oral administration, Cimetidine Capsules are rapidly absorbed in the gastrointestinal tract with a bioavailability of 60% -70%. Its peak time (Tmax) is 1-3 hours, and it can take effect within 30 minutes after oral administration, making it a rapid relief drug for acute gastric acid reflux symptoms. Food can slow down its absorption rate but does not affect the degree of absorption, so patients do not need to strictly take medication on an empty stomach. It is worth noting that when used in combintion with medicine such as sucralfate and metoclopramide, the absorption of Cimetdine may decrease or decrease, and the dosing interval or dosis needs to be adjusted.
Cimetdine is widely distributed in the body, with an apparent distribution volume (Vd) of 0.8-1.2 L/kg, and can penetrate into bodily fluids such as saliva, breast milk, and cerebrospinal fluid. Its protein binding rate is about 20%, and the concentrtion of free drug is relatively high, which explains the mechanism by which it may cause central nervous system side effects after penetrating the blood-brain barrier. In animal experiments, Cimetdine can cross the placental barrier, but preclinical studies have not shown teratogenicity.
Cimetdine is a potent inhibitor of the CYP450 enzyme system, particularly exhibiting significant inhibitory effects on CYP1A2, CYP2D6, and CYP3A4 subtypes. This inhibitory effect leads to a slowdown in its own metabolism, with a half-life (T1/2) extended to 2-3 hours. Meanwhile, Cimetdine induces multiple drug interactions by inhibiting the metabolism of other medicine
Warfarin: When used in combintion, the INR value increases by 30% -50%, and the dose of warfarin needs to be reduced by 25% -50%.
Phenytoin Sodium: Blood concentrtion has increased by 28%, and the dosis needs to be adjusted to the lower limit of the tratment range.
Lidocaine: clerance rate reduced by 34%, maintenance dose needs to be reduced by 20% -30%.
Theophylline: When used in combintion, the blood concentrtion of theophylline increases by 50% -100%. It is necessary to monitor the blood concentrtion of theophylline and adjust the dosis.
Cimetdine is mainly excreted through the kidneys, with 60% -70% excreted in its original form through urine and 20% -30% excreted through bile. In animal models of renal insufficiency, its clerance rate significantly decreases and its half-life extends to 4-6 hours. Therefore, the dosis needs to be adjusted according to creatinine clerance rate:
Mild renal insufficiency (CrCl 50-80 mL/min): No dose adjustment required.
Moderate renal insufficiency (CrCl 30-50 mL/min): Reduce the dosis by 50% each time and extend the dosing interval to 12 hours.
Severe renal insufficiency (CrCl<30 mL/min): contraindicated or requiring hemodialysis support.
Pharmacological mechanism: H2 receptor antagonism and multi-target effects
1. Core mechanism: Competitive antagonism of H2 receptors
Cimetdine, as a first generation H2 receptor antagonist, blocks histamine induced gastric acid secretion by competitively binding to H2 receptors on the basal membrane of gastric wall cells. Its functional characteristics include:
Comprehensively inhibit gastric acid secretion: not only does it reduce basal gastric acid secretion (by 50% -70% during nighttime acid breakthrough), but it can also inhibit gastric acid secretion induced by stimuli such as food, histamine, pentagastrin, caffeine, etc.
Gastric mucosal protection: By reducing the erosion of gastric acid on the gastric mucosa, promoting ulcer healing, the healing rate of duodenal ulcers can reach 80% -90%.
Stress ulcer prevention: In animal models of intensive care, the incidence of stress ulcers can be reduced by 30% -50%.
2. Expansion effect: anti androgen and immune regulation
(1) Antiandrogenic effect
High dose Cimetdine (≥ 1.2 g/d) can competitively bind to androgen receptors and produce weak anti androgen effects:
Preclinical studies: In animal models, Cimetdine can reduce epididymal weight and sperm count in male rats, but does not affect serum testosterone levels.
Clinical application: It was once used to treat hirsutism in women, but its efficacy was weaker than spironolactone, and it is now rarely used.
(2) Immune regulatory effect
Cimetdine exhibits potential in tumor adjuvant therapy by inhibiting T lymphocyte activation and enhancing natural killer (NK) cell activity
Gastric cancer:
Combined with chemotherapy can increase the 1-year survival rate by 15% -20%.
Melanoma:
Postoperative adjuvant therapy can reduce the recurrence rate by 25%.
Viral skin disease:
Combined tratment with acyclovir can shorten the course of herpes zoster by 3-5 days.
adverse reaction
1. Common symptoms include diarrhea, nausea, vomiting, abdominal distension, constipation, bitter mouth, dry mouth, mild elevation of serum aminotransferase, and occasionally severe hepatitis, liver necrosis, and hepatic steatosis. For patients with cirrhosis, it may induce hepatic encephalopathy. Sudden discontinuation of medication may cause chronic peptic ulcer perforation, estimated to be caused by high acidity rebound after discontinuation. There are also reports that cimetdine can cause acute pancreatitis.
2. Hematological system: Cimetidine capsules has a certain inhibitory effect on bone marrow, which can lead to neutropenia and pancytopenia; There are also reports of thrombocytopenia and granulocyte deficiency; Only individual cases have been reported to present with autoimmune hemolytic anemia, aplastic anemia, and eosinophilia. Adverse reactions of cimetdine in the blood system are more common in patients with severe complications, or those receiving anti metabolic hydrocarbon medicine or other tratments that lead to granulocytopenia.
3. Neurological/Mental System
(1) Dizziness, headache, fatigue, drowsiness, and other symptoms are common. A small number of patients may experience reversible confusion, disorientation, restlessness, sensory delay, unclear language, local seizures or epileptic seizures, delirium, depression, hallucinations, extrapyramidal reactions, and motor polyneuropathy. After the occurrence of neurotoxic symptoms, it is generally only necessary to reduce the dosis of medication appropriately to disappear, or it can be treated with the cholinergic drug sophocarpine.
(2) When treating gastrointestinal complications of alcoholism, tremulous delirium may occur, similar to alcohol withdrawal syndrome, and attention should be paid to distinguishing it.
(3) The neurological and psychiatric adverse reactions of cimetdine mainly occur in critically ill patients, elderly patients, young children, those with liver and kidney dysfunction, those with a history of mental illness, those with brain diseases, and those who take high-dose medication. In addition, individuals with pseudo hypothyroidism may be more sensitive to the neurotoxic effects of cimetdine.
4. Endocrine/metabolic system: Cimetdine has mild anti androgenic effects and can cause lipid metabolism abnormalities, hyperprolactinemia, decreased plasma testosterone levels and increased gonadotropin levels, male breast development and breast tenderness, as well as female galactorrhea.
5. Cardiovascular system: bradycardia, facial flushing, etc. may occur. During intravenous injection, occasional drops in blood pressure, premature atrial contractions, cardiac and respiratory arrest, etc.
6. Urinary/reproductive system:
(1) Cimetdine can cause transient increase in serum creatinine levels and decrease in creatinine clerance rate, and its mechanism is competition with creatinine for renal tubular secretion. There are also reports of acute renal dysfunction, which can be restored to normal after discontinuation of medication.
(2) Interstitial nephritis: It can disappear after discontinuation of medication.
(3) Sexual dysfunction: High doses of medication (above 1.6g per day) can cause erectile dysfunction, decreased libido, decreased sperm count, etc., but can be restored to normal after discontinuation of medication.
(4) Tratment with cimetdine in patients with renal allogeneic transfer can lead to acute necrosis of metastases
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