Famotidine is metabolized in the liver to famotidine S-oxide (S-famotidine). The metabolite does not appear to inhibit gastric acid secretion. Orally administered famotidine undergoes minimal metabolism on first pass through the liver.
Chronic therapy with famotidine has been associated with minor elevations in serum aminotransferase levels in 1% to 4% of patients, but similar rates were reported in placebo recipients. The ALT elevations are usually asymptomatic and transient, and may resolve without dose modification. Rare instances of clinically apparent liver injury have been reported in patients receiving famotidine, but few cases have been reported and clinical characteristics in published cases have varied in the time to onset and pattern of injury. Onset has ranged from 1 to 14 weeks and serum enzyme pattern has typically been hepatocellular. The injury resolves within 4 to 12 weeks of stopping famotidine. Immunoallergic features (rash, fever, eosinophilia) are uncommon, as is autoantibody formation.
◉ Summary of Use during Lactation:Famotidine doses in breastmilk result in infant dosages that are lower than those used in newborn infants. Famotidine would not be expected to cause any adverse effects in breastfed infants. No special precautions are required.
◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk:Histamine H2-receptor blockade is known to stimulate prolactin secretion. Oral famotidine usually does not affect serum prolactin levels, but rare cases of hyperprolactinemia and galactorrhea have been reported. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.
◈ What is famotidine?
Famotidine is a medication used to treat acid reflux (sometimes called heartburn) or peptic ulcer disease. Famotidine reduces the amount of stomach acid that your body makes. It is a long-acting histamine (H2) receptor blocker. Some brand names are Pepcid®, Pepcid AC®, and Heartburn Relief®.Sometimes when people find out they are pregnant, they think about changing how they take their medication, or stopping their medication altogether. However, it is important to talk with your healthcare providers before making any changes to how you take this medication. Your healthcare providers can talk with you about the benefits of treating your condition and the risks of untreated illness during pregnancy.
◈ I take famotidine. Can it make it harder for me to get pregnant?
Studies have not been done to see if taking famotidine could make it harder to become pregnant.
◈ Does taking famotidine during my pregnancy increase the chance for miscarriage?
Miscarriage is common and can occur in any pregnancy for many different reasons. It is not known if famotidine could increase the chance for miscarriage.
◈ Does taking famotidine increase the chance for birth defects?
Every pregnancy starts out with a 3-5% chance of having a birth defect. This is called the background risk. Available studies do not show an increased chance of birth defects when famotidine is taken during pregnancy.
◈ Does taking famotidine increase the chance of other pregnancy complications?
It is not known if taking famotidine during pregnancy increases the chance of pregnancy complications. However, studies on the overall class of medications called H2 receptor blockers did not find pregnancy-related problems, such as preterm delivery (birth before week 37) or low birth weight (weighing less than 5 pounds, 8 ounces [2500 grams] at birth).
◈ Does taking famotidine during pregnancy affect future behavior or learning for the child?
It is not known if taking famotidine during pregnancy affects children’s long-term development. One study looked at famotidine use in pregnancy and did not find an increased chance of asthma when the children were 2 years old.
◈ Breastfeeding while taking famotidine:
Famotidine gets into breast milk in small amounts and is used in newborn infants in higher dosages than the levels that have been found in breastmilk. Taking famotidine while breastfeeding is not expected to cause problems in breastfed infants. Be sure to talk to your healthcare provider about all of your breastfeeding questions.
◈ If a male takes famotidine, could it affect fertility (ability to get partner pregnant) or increase the chance of birth defects?
One study reported that taking famotidine did not affect hormones in males; this makes it less likely that famotidine could affect fertility. In general, exposures that fathers or sperm donors have are unlikely to increase the risks to a pregnancy. For more information, please see the MotherToBaby fact sheet Paternal Exposures at https://mothertobaby.org/fact-sheets/paternal-exposures-pregnancy/.
来源:Mother To Baby Fact Sheets
毒理性
副作用
职业性肝毒素 - 第二性肝毒素：在职业环境中的毒性效应潜力是基于人类摄入或动物实验的中毒病例。
Occupational hepatotoxin - Secondary hepatotoxins: the potential for toxic effect in the occupational setting is based on cases of poisoning by human ingestion or animal experimentation.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
Concurrent use /of antacids/ with histamine H2-receptor antagonists in the treatment of peptic ulcer may be indicated for the relief of pain; however, simultaneous administration of antacids of medium to high potency (80 mmol to 150 mmol HCl) is not recommended since absorption of histamine H2-receptor antagonists may be decreased; patients should be advised not to take any antacids within 1/2 to 1 hour of histamine H2-receptor antagonists. /Histamine H2-receptor antagonists/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
所有H2受体拮抗剂都分布在母乳和脑脊液中。/组胺H2受体拮抗剂/
All H2-receptor antagonists are distributed in breast milk and cerebral spinal fluid. /Histamine H2-receptor antagonists/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
famotidine在人体组织和液体中的分布尚未得到充分表征。据报道，该药物的表观分布体积为1.1-1.4 l / kg，在成人中，并且似乎在肾功能损害的患者中并未显著改变。在大鼠口服或静脉注射后，法莫替丁广泛分布，在肾脏，肝脏，胰腺和下颌下腺中浓度最高。该药物的蛋白结合率为15-20％。
Distribution of famotidine into human body tissues and fluids has not been fully characterized. The apparent volume of distribution of the drug is reported to be 1.1-1.4 l/kg in adults and does not appear to be altered substantially in patients with renal dysfunction. Following oral or IV administration in rats, famotidine is widely distributed, appearing in highest concentrations in the kidney, liver, pancreas, and submandibular gland. The drug is 15-20% protein bound.
In rats famotidine appears to distribute only minimally into the CNS, and does not cross the placenta. It is not known whether the drug crosses the placenta in humans. Famotidine is distributed into milk in rats; however, it is not known whether the drug is distributed into milk in humans.
Famotidine is excreted principally in urine via glomerular filtration and tubular secretion. Approximately 25-30 or 65-80% of a dose is excreted unchanged in urine within 24 hours following oral or IV administration, respectively, and approximately 13-49 or 52-82% of a single 40 mg oral or IV dose respectively, is excreted within 72 hours. ... The remainder of an orally administered dose is eliminated in feces.
Substituted 1,3-thiazole compounds, their production and use
申请人：——
公开号：US20040053973A1
公开（公告）日：2004-03-18
(1) A 1,3-thiazole compound of which the 5-position is substituted with a 4-pyridyl group having a substituent including no aromatic group or (2) a 1,3-thiazole compound of which the 5-position is substituted with a pyridyl group having at the position adjacent to a nitrogen atom of the pyridyl group a substituent including no aromatic group has an excellent p38 MAP kinase inhibitory activity.
A stabilized preparation which comprises: a unstable drug in a polyethylene glycol-containing preparation; and a coating agent comprising a copolyvidone instead of polyethylene glycol with which the drug is coated.
This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula (I) wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
ANTHELMINTIC COMPOUNDS AND COMPOSITIONS AND METHOD OF USING THEREOF
申请人：Meng Charles Q.
公开号：US20140142114A1
公开（公告）日：2014-05-22
The present invention relates to novel anthelmintic compounds of formula (I) below:
wherein
Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X
1
, X
2
, X
3
, X
4
, X
5
, X
6
, X
7
and X
8
are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.
This invention relates to compounds of the formula (I):
wherein R
1
, R
2
, R
3
, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT
4
receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
