Its derivatives include Colforsin, NKH477 and FSK88 which might be potent than forskolin at raising cAMP. They might be useful ... Wajima Z, Yoshikawa T, Ogura A, Imanaga K, Shiga T, Inoue T, Ogawa R (April 2002). "Intravenous colforsin daropate, a water- ...
... colforsin (INN) colfosceril palmitate (INN) Colgate Total colimecycline (INN) colistimethate sodium (INN) colistin (INN) ...
The molecular formula C27H43NO8 (molar mass: 509.631 g/mol, exact mass: 509.2989 u) may refer to: Colforsin Veracevine This set ...
... (INN) is a water-soluble derivative of forskolin. Mori M, Takeuchi M, Takaoka H, Hata K, Hayashi Y, Yokoyama M ( ...
The official start to its development started in December 1986 when Merck's president, Edward Scolnick, announced that they would start a comprehensive AIDS research program. They started a laboratory dedicated to AIDS research in West Point, Pennsylvania and placed Emilio Emini in charge of the laboratory.[11] A couple months later on January, 1987, a team of researchers consisting of Emilio Emini, Joel Huff, and Irving Sigal, kickstarted their studies by basing their project off of earlier research on the protease enzyme, renin.[5] They were the ones who started the process of research and development into protease inhibitors and its relation to the virus. Over a year later, in July 1988, Nancy Kohl, Emilio Emini, et al., published in the Proceedings of the National Academy of the Science about the idea of inhibiting the protease.[11] On February, 1989, Manuela Navia, Paula Fitzgerald, et al., published a paper that showed the three-dimensional structure of HIV's protease enzyme.[5] Other ...
... is typically used to treat hypothyroidism,[9] and is the treatment of choice for people with hypothyroidism,[10] who often require lifelong thyroid hormone therapy.[11] It may also be used to treat goiter via its ability to lower thyroid-stimulating hormone (TSH), a hormone that is considered goiter-inducing.[12][13] Levothyroxine is also used as interventional therapy in people with nodular thyroid disease or thyroid cancer to suppress thyroid-stimulating hormone (TSH) secretion.[14] A subset of people with hypothyroidism treated with an appropriate dose of levothyroxine will describe continuing symptoms despite TSH levels in the normal range.[11] In these people, further laboratory and clinical evaluation is warranted as they may have another cause for their symptoms.[11] Furthermore, it is important to review their medications and possible dietary supplements as several medications can affect thyroid hormone levels.[11] Levothyroxine is also used to treat subclinical ...
... is a low cost drug.[7] In the United States, Salix Pharmaceuticals holds a US Patent for rifaximin and markets the drug under the name Xifaxan.[17][18] In addition to receiving FDA approval for traveler's diarrhea and (marketing approved for)[18] hepatic encephalopathy, rifaximin received FDA approval for IBS in May 2015.[19] No generic formulation is available in the US and none has appeared due to the fact that the FDA approval process was ongoing. If rifaximin receives full FDA approval for hepatic encephalopathy it is likely that Salix will maintain marketing exclusivity and be protected from generic formulations until March 24, 2017.[18] Rifaximin is approved in 33 countries for GI disorders.[20][21] On August 13, 2013, Health Canada issued a Notice of Compliance to Salix Pharmaceuticals Inc. for the drug product Zaxine.[22] In India it is available under the brand names Ciboz and Xifapill.[citation needed] In Russia and Ukraine the drug is sold under the name Alfa Normix ...
Long-term use of methylprednisolone, as with all corticosteroids, can be associated with hyperglycemia, decreased resistance to infection, swelling of face, weight gain, congestive cardiac insufficiency, fluid and sodium retention, edema, hypertension, increased eye pressure, glaucoma, osteoporosis, and psychosis, especially when used at high doses.[11][12] The most serious side effect occurs after the adrenal glands cease natural production of cortisol, which methylprednisolone will replace. Abrupt cessation of the drug after this occurs can result in a condition known as Addisonian crisis, which can be fatal. To prevent this, the drug is usually prescribed with a tapering dose, including a predosed "dose pack" detailing a specific number of tablets to take at designated times over a several-day period. Pharmacists sometimes advise that this drug may cause sleeplessness and "down" moods. Measles and chicken pox are very dangerous and potentially fatal for people on methylprednisolone therapy. ...
Important drug interactions are rare.[27][28] However, the most significant major drug interaction concern is the decreased activation of clopidogrel when taken together with omeprazole.[29] Although still controversial,[30] this may increase the risk of stroke or heart attack in people taking clopidogrel to prevent these events. This interaction is possible because omeprazole is an inhibitor of the enzymes CYP2C19 and CYP3A4.[31] Clopidogrel is an inactive prodrug that partially depends on CYP2C19 for conversion to its active form. Inhibition of CYP2C19 may block the activation of clopidogrel, which could reduce its effects.[32][33] Almost all benzodiazepines are metabolised by the CYP3A4 and CYP2D6 pathways, and inhibition of these enzymes results in a higher AUC (i.e., the total effect over time of a given dose). Other examples of drugs dependent on CYP3A4 for their metabolism are escitalopram,[34] warfarin,[35] oxycodone, tramadol, and oxymorphone. The concentrations of these drugs may ...
Bonow RO, Carabello BA, Kanu C, et al. (August 2006). "ACC/AHA 2006 guidelines for the management of patients with valvular heart disease: a report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (writing committee to revise the 1998 Guidelines for the Management of Patients With Valvular Heart Disease): developed in collaboration with the Society of Cardiovascular Anesthesiologists: endorsed by the Society for Cardiovascular Angiography and Interventions and the Society of Thoracic Surgeons". Circulation. 114 (5): e84-231. doi:10.1161/CIRCULATIONAHA.106.176857. PMID 16880336 ...
... has been investigated for use as a radiation countermeasure. Its value as a radiation countermeasure is based mainly on its stimulation of production of white blood cells and platelets.[6] Its potential use as a radiation countermeasure was developed by the Armed Forces Radiobiology Research Institute (AFRRI) and subsequently studied by AFRRI and Hollis-Eden Pharmaceuticals under the proposed brand name Neumune for the treatment of acute radiation syndrome.[6][7] The clinical trials with rhesus monkeys were successful. According to the Hollis-Eden report, only 12.5% of the 40 Neumune-treated animals died versus 32.5% in the placebo group.[8] Hollis-Eden had applied for a contract from the U.S. Government under the BioShield Request for Proposals (RFP) for radiation countermeasures. After being encouraged for 2.5 years that Neumune was in the competitive range, on March 9, 2007, the RFP was canceled by HHS. According to HHS, "the product was no longer in the competitive ...
... (CBZ), sold under the trade name Tegretol among others, is an anticonvulsant medication used primarily in the treatment of epilepsy and neuropathic pain.[1] It is not effective for absence or myoclonic seizures.[1] It is used in schizophrenia along with other medications and as a second-line agent in bipolar disorder.[3][1] Carbamazepine appears to work as well as phenytoin and valproate for focal and generalised seizures.[4] Common side effects include nausea and drowsiness.[1] Serious side effects may include skin rashes, decreased bone marrow function, suicidal thoughts, or confusion.[1] It should not be used in those with a history of bone marrow problems.[1] Use during pregnancy may cause harm to the baby; however, stopping the medication in pregnant women with seizures is not recommended.[1] Its use during breastfeeding is not recommended.[1] Care should be taken in those with either kidney or liver problems.[1] Carbamazepine was discovered in 1953 by Swiss chemist Walter ...
... is an allosteric endocannabinoid, as it is a negative allosteric modulator of the CB1 receptor.[4][5] Pregnenolone is involved in a natural negative feedback loop against CB1 receptor activation in animals.[6][better source needed] It prevents CB1 receptor agonists like tetrahydrocannabinol, the main active constituent in cannabis, from fully activating the CB1 [6][better source needed] Pregnenolone has been found to bind with high, nanomolar affinity to microtubule-associated protein 2 (MAP2) in the brain.[7][8] In contrast to pregnenolone, pregnenolone sulfate did not bind to microtubules.[7][8] However, progesterone did and with similar affinity to pregnenolone, although unlike pregnenolone, it did not increase binding of MAP2 to tubulin.[7][8] Pregnenolone was found to induce tubule polymerization in neuronal cultures and to increase neurite growth in PC12 cells treated with nerve growth factor.[7][8] As such, pregnenolone may control formation and stabilization of microtubules ...
... has little systemic absorption, and is considered safe for topical use in adults and children over the age of 2 months. The FDA has assigned it as pregnancy category B. Animal studies have shown no effects on fertility or teratogenicity, but studies in humans have not been performed. The excretion of permethrin in breastmilk is unknown, and breastfeeding is recommended to be temporarily discontinued during treatment.[11] According to the Connecticut Department of Public Health, permethrin "has low mammalian toxicity, is poorly absorbed through the skin, and is rapidly inactivated by the body. Skin reactions have been uncommon."[14] Excessive exposure to permethrin can cause nausea, headache, muscle weakness, excessive salivation, shortness of breath, and seizures. Worker exposure to the chemical can be monitored by measurement of the urinary metabolites, while severe overdose may be confirmed by measurement of permethrin in serum or blood plasma.[15] Permethrin does not present any ...
where CL is total body clearance (L/h), BSA is total body surface area (m2), AAG and ALB represent alpha1 acid glycoprotein and albumin plasma concentrations (g/L) respectively, and AGE is the patients age (years).[13] HEP12 represents a measure of hepatic dysfunction, affecting clearance of docetaxel. This final model accounted for a modest proportion of patients and identified most of the patients varying from the model (population median of CL = 35.6 L/h) as having hepatic dysfunction, indicating hepatic function as the most unpredictable factor with regards to clearance variability.[13] Patients with significant hepatic dysfunction had an approximately 30% decrease in clearance of docetaxel and were also at a higher risk of toxicity poisoning from docetaxel treatment.[13] Clearance has been shown from population pharmacokinetic studies to decrease significantly with age, increased alpha1 acid glycoprotein and albumin concentrations and decreased body surface area.[13] Renal impairment is ...
InChI=1S/C22H22N2O8/c1-7-8-5-4-6-9(25)11(8)16(26)12-10(7)17(27)14-15(24(2)3)18(28)13(21(23)31)20(30)22(14,32)19(12)29/h4-6,10,14-15,17,25,27-29,32H,1H2,2-3H3,(H2,23,31)/t10-,14-,15+,17+,22+/m1/s1 ...
Human exposure to methoxychlor occurs via air, soil, and water,[7] primarily in people who work with the substance or who are exposed to air, soil, or water that has been contaminated. It is unknown how quickly and efficiently the substance is absorbed by humans who have been exposed to contaminated air or via skin contact.[7] In animal models, high doses can lead to neurotoxicity.[7] Some methoxychlor's metabolites have estrogenic effects in adult and developing animals before and after birth.[7] One studied metabolite is 2,2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane (HPTE) which shows reproductive toxicity in an animal model by reducing testosterone biosynthesis.[8][9] Such effects adversely affect both the male and female reproductive systems. It is expected that this "could occur in humans" but has not been proven.[7] While one study has linked methoxychlor to the development of leukemia in humans, most studies in animals and humans have been negative, thus the EPA has determined that it is ...
... , also known as eltanolone (INN), is an endogenous neurosteroid that is biosynthesized from progesterone.[1] It is a positive allosteric modulator of the GABAA receptor,[1] as well as a negative allosteric modulator of the glycine receptor,[2] and is known to have sedative, anxiolytic, anesthetic, and anticonvulsant effects.[1][2][3] It was investigated for clinical use as a general anesthetic, but produced unwanted side effects such as convulsions on occasion, and for this reason was never marketed.[2][4] During pregnancy, pregnanolone and allopregnanolone are involved in sedation and anesthesia of the fetus.[5][6] ...
As of 2017 brands included: Actalor, Actidin, Aerotina, Alaspan, Alavert, Albatrina, Alerdina, Alerfast, Alergan, Alergiano, Alergiatadina, Alergin Ariston, Alergipan, Alergit, Alergitrat L, Aleric Lora, Alermuc, Alernitis, Alerpriv, Alertadin, Alertine, Aleze, Algac, Algecare, Algistop, Alledryl, Aller-Tab, Allerfre, Allerget, Allergex Non Drowsy, Allergyx, Allerhis, Allernon, Allerta, Allertyn, Allohex, Allor, Allorat, Alloris, Alor, Analor, Anhissen, Anti-Sneeze, Antial, Antil, Antimin, Ao Hui Feng, Ao Mi Xin, Ao Shu, Ardin, Atinac, Avotyne, Axcel Loratadine, Bai Wei Le, Bang Nuo, Bedix, Belodin, Benadryl, Besumin, Bi Sai Ning, Bi Yan Tong, Biliranin, Biloina, Biolorat, Bollinol, Boots Hayfever Relief, Boots Hooikoortstabletten, Boots Once-a-Day Allergy Relief, Carin, Carinose, Chang Ke, Civeran, Clara, Claratyne, Clarid, Clarihis, Clarihist, Clarilerg, Clarinese, Claritin, Claritine, Clarityne, Clarityne SP, Clarotadine, Clatatin, Clatine, Clear-Atadine, Clear-Atadine Children's, Clistin, ...
A component in various medicinal plants (e.g. Scutellaria baicalensis), chrysin is a dihydroxyflavone, a type of flavonoid.[6] It is also found in honey, propolis, the passion flowers, Passiflora caerulea and Passiflora incarnata, in Oroxylum indicum,[2] carrots,[1] chamomile,[7] many fruits, and in mushrooms, such as the mushroom, Pleurotus ostreatus.[6] It is extracted from various plants,[1] such as the blue passion flower (Passiflora caerulea).[1] The amount of chrysin in honey from various plant sources is about 0.2 mg per 100 g.[8] Chrysin is typically found at higher amounts in propolis than in honey.[9] A 2010 study found the amount of chrysin was 0.10 mg/kg in honeydew honey, and 5.3 mg/kg in forest honeys.[10] A 2010 study found the amount of chrysin in propolis was as much as 28 g/L.[10] A 2013 study found the amount of chrysin in various mushrooms from the island of Lesvos, Greece varied between 0.17 mg/kg in Lactarius deliciosus to 0.34 mg/kg in Suillus bellinii.[10] ...
Recreational use of tianeptine is rare[according to whom?] and thus far has only been seen in persons already using multiple substances for recreational purposes.[citation needed] In 2001, Singapore's Ministry of Health restricted tianeptine prescribing to psychiatrists due to its recreational potential,[49] In 2003, Bahrain classified it a controlled substance due to increasing reports of misuse and recreational use.[50] Between 1989 and 2004, in France 141 cases of recreational use were identified, correlating to an incidence of 1 to 3 cases per 1000 persons treated with tianeptine and 45 between 2006 and 2011. The main reason for recreational use is to achieve an anxiolytic effect. According to Servier, stopping of treatment with tianeptine is difficult, due to the possibility of withdrawal symptoms in a person. The severity of the withdrawal is dependent on the daily dose, with high doses being extremely difficult to quit.[51][better source needed][52][53] In 2007, according to French Health ...
... is very toxic to cats which cannot tolerate the therapeutic doses for dogs.[7] This is associated with UGT1A6 deficiency in cats, the enzyme responsible for metabolizing cypermethrin. As a consequence, cypermethrin remains much longer in the cat's organs than in dogs or other mammals and can be fatal in large doses. In male rats cypermethrin was shown to exhibit a toxic effect on the reproductive system. After 15 days of continual dosing, both androgen receptor levels and serum testosterone levels were significantly reduced. These data suggested that cypermethrin can induce impairments of the structure of seminiferous tubules and spermatogenesis in male rats at high doses.[8] Long-term exposure to cypermethrin during adulthood is found to induce dopaminergic neurodegeneration in rats, and postnatal exposure enhances the susceptibility of animals to dopaminergic neurodegeneration if rechallenged during adulthood.[9] If exposed to cypermethrin during pregnancy, rats give birth to ...
Biosynthesis of mevastatin is primarily accomplished via a type 1 PKS pathway it proceeds in the PKS pathway as seen in figure 1 until it reaches a hexaketide state where it undergoes a Diels-Alder cyclization. After cyclization it continues via the PKS pathway to a nonaketide after which it is released and undergoes oxidation and dehydration. It is presumed that the oxidations are preformed by a polypeptide that is similar to cytochrome p450 monooxygenase, which is encoded by mlcC within the mevastatin gene. Lastly the biosynthesis is completed by the PKS facilitating the addition of a diketide sidechain and a methylation by SAM.[7] Figure 1 shows mevastatin in its acid form but it can also be in the more commonly seen lactone form. This pathway was first observed in Penicillium cilrinum and was later discovered that another type of fungus, Penicillium brevicompaetum also produced mevastatin via a PKS pathway. ...
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It is commonly available without a prescription in various dosage forms, such as a topical cream, ointment, or vaginal suppository. It is also available as an oral troche or throat lozenge as a prescription only. Topically, clotrimazole is used for vulvovaginal candidiasis (yeast infection) or yeast infections of the skin. For vulvovaginal candidiasis (yeast infection), clotrimazole tablets and creams are inserted into the vagina. Topical clotrimazole is usually not effective in treatment of fungal infections of the scalp or nails.[citation needed] When using over-the-counter drug clotrimazole products, use should be discontinued if condition does not improve after treatment for 2 weeks for jock itch or after 4 weeks for athlete's foot or ringworm.[6] Throat lozenge preparations are used for oropharyngeal candidiasis (oral thrush) or prevention of oral thrush in people with neutropenia.[6] Clotrimazole is usually used 5 times daily for 14 days for oral thrush, twice daily for 2 to 8 weeks for ...
... (5α-DHP), also known as allopregnanedione,[1] as well as 5α-pregnane-3,20-dione, is an endogenous progestogen and neurosteroid that is synthesized from progesterone.[2][3] It is also an intermediate in the synthesis of allopregnanolone and isopregnanolone from progesterone. 5α-DHP is an agonist of the progesterone receptor and a positive allosteric modulator of the GABAA receptor (albeit with an affinity for this receptor that is regarded as relatively low (in comparison to 3α-hydroxylated progesterone metabolites such as allopregnanolone and pregnanolone)).[2][3][4][5] It has also been found to act as a negative allosteric modulator of the GABAA-rho receptor.[6] In addition, it is a weak agonist of the pregnane X receptor (PXR) (EC50 ,10,000 µM)), with approximately six-fold lower potency relative to its 5β-isomer, 5β-dihydroprogesterone.[7]. ...
... has a potential for drug interactions; caution should be used in combining other medicines with it, including other antiepileptics and mood stabilizers.[12] Lower levels of carbamazepine are seen when administrated with phenobarbital, phenytoin, or primidone, which can result in breakthrough seizure activity. Carbamazepine, as a CYP450 inducer, may increase clearance of many drugs, decreasing their concentration in the blood to subtherapeutic levels and reducing their desired effects.[19] Drugs that are more rapidly metabolized with carbamazepine include warfarin, lamotrigine, phenytoin, theophylline, and valproic acid.[12] Drugs that decrease the metabolism of carbamazepine or otherwise increase its levels include erythromycin,[20] cimetidine, propoxyphene, and calcium channel blockers.[12] Carbamazepine also increases the metabolism of the hormones in birth control pills and can reduce their effectiveness, potentially leading to unexpected pregnancies.[12] As a drug that induces ...
... (Gewodin, Gewolen) is a nonsteroidal anti-inflammatory agent (NSAID) of the pyrazolone series which is available over-the-counter in some countries such as Taiwan.[1][2][3] It has analgesic, anti-inflammatory, and antipyretic effects.[1][2] Famprofazone has been known to produce methamphetamine as an active metabolite, with 15-20% of an oral dose being converted to it.[4][5] As a result, famprofazone has occasionally been implicated in causing positives on drug tests for amphetamines.[3] ...
... is considered a prohormone in the formation of dehydroepiandrosterone (DHEA), itself a prohormone of the sex steroids. This conversion is mediated by the enzyme 17,20 lyase. As such 17α-hydroxypregenolone represents an intermediary in the Δ5 pathway that leads from pregnenolone to DHEA. 17α-Hydroxypregneolone is also converted to 17α-hydroxyprogesterone, a prohormone for glucocorticosteroids and androstenedione through the activity of 3α-hydroxysteroid dehydrogenase. ...
... is available as a generic medication and usually not too expensive.[7] Wholesale it costs between US$0.003 and US$0.15 per dose.[8] A month of treatment is about US$30 in the United States.[2] Since September 2012, the marketing licence in the UK has been held by Flynn Pharma Ltd, of Dublin, Ireland, and the product, although identical, has been called Phenytoin Sodium xxmg Flynn Hard Capsules. (The xxmg in the name refers to the strength-for example "Phenytoin sodium 25 mg Flynn Hard Capsules").[49] The capsules are still made by Pfizer's Goedecke subsidiary's plant in Freiburg, Germany and they still have Epanutin printed on them.[50] After Pfizer's sale of the UK marketing licence to Flynn Pharma, the price of a 28-pack of 25 mg phenytoin sodium capsules marked Epanutin rose from 66p (about $0.88) to £15.74 (about $25.06). Capsules of other strengths also went up in price by the same factor-2384%,[51] costing the UK's National Health Service an extra £43 million (about $68.44 ...