Therapeutic uses: All types of hyperlipidemias.
... orally. Pravastatin and fluvastatin are almost completely absorbed after oral administration; Similarly, Fluvastatin and pravastatin are active as such, whereas lovastatin and simvastatin must be hydrolyzed to their acid forms. Due to first-pass metabolism, the primary action of these drugs is on th ...
... orally. Pravastatin and fluvastatin are almost completely absorbed after oral administration; Similarly, Fluvastatin and pravastatin are active as such, whereas lovastatin and simvastatin must be hydrolyzed to their acid forms. Due to first-pass metabolism, the primary action of these drugs is on th ...
Hydrochloric acid
... sensation, chronic cough and hoarsenes), due to reflux of stomach contents into esophagus. • Mucosal injury may present or not. • It is a very common disorder affecting between 1030% of western population. • Especially common in pregnant women and obese people. ...
... sensation, chronic cough and hoarsenes), due to reflux of stomach contents into esophagus. • Mucosal injury may present or not. • It is a very common disorder affecting between 1030% of western population. • Especially common in pregnant women and obese people. ...
The lead compound
... binding of a compound to a receptor. • Potency - concentration of an agonist required to produce 50% of the maximum possible effect. ...
... binding of a compound to a receptor. • Potency - concentration of an agonist required to produce 50% of the maximum possible effect. ...
An Introduction to Medicinal Chemistry
... This text is aimed at undergraduates who have a basic grounding in chemistry and are interested in a future career in the pharmaceutical industry. It attempts to convey something of the fascination of working in a field which overlaps the disciplines of chemistry, biochemistry, cell biology, and pha ...
... This text is aimed at undergraduates who have a basic grounding in chemistry and are interested in a future career in the pharmaceutical industry. It attempts to convey something of the fascination of working in a field which overlaps the disciplines of chemistry, biochemistry, cell biology, and pha ...
Biron_JSBMB_2015_rev - Corpus UL
... Like other NRs, the AR displays a modular structure composed of an N-terminal domain (NTD) bearing the activation function (AF) 1, a DNA-binding domain (DBD), a connecting hinge region containing a nuclear localization signal (NLS) and a C-terminal ligand-binding domain (LBD) (Fig. 1). The LBD is co ...
... Like other NRs, the AR displays a modular structure composed of an N-terminal domain (NTD) bearing the activation function (AF) 1, a DNA-binding domain (DBD), a connecting hinge region containing a nuclear localization signal (NLS) and a C-terminal ligand-binding domain (LBD) (Fig. 1). The LBD is co ...
Section 4.5: Interaction with other medicinal products and
... Transporter interactions: Amiodarone, verapamil and clarithromycin are inhibitors of the efflux transporter Pglycoprotein and active substance X is a substrate of this transporter. Amiodarone: When active substance X was coadministered with a single oral dose of 600 mg amiodarone, the extent and rat ...
... Transporter interactions: Amiodarone, verapamil and clarithromycin are inhibitors of the efflux transporter Pglycoprotein and active substance X is a substrate of this transporter. Amiodarone: When active substance X was coadministered with a single oral dose of 600 mg amiodarone, the extent and rat ...
diuretics
... explain this effect postulates that thiazide diuretics act directly on vascular smooth muscle to facilitate opening of a Ca2+-dependent K+ channel (i.e., a K+ channel whose opening is stimulated by increased cytoplasmic Ca2+ concentration). Opening of these channels hyperpolarizes the smooth muscle ...
... explain this effect postulates that thiazide diuretics act directly on vascular smooth muscle to facilitate opening of a Ca2+-dependent K+ channel (i.e., a K+ channel whose opening is stimulated by increased cytoplasmic Ca2+ concentration). Opening of these channels hyperpolarizes the smooth muscle ...
CYTOCHROME P450 3A4 IS THE MAJOR ENZYME RESPONSIBLE
... N-deethylation and the hydroxylation in the aniline part of the molecule constituted about 19, 10, and 4%, respectively (Fig. 3). Correlation of Laquinimod Metabolism toward Other Specific P450 Activities across a Panel of Human Livers. Laquinimod metabolism was determined in microsomal preparations ...
... N-deethylation and the hydroxylation in the aniline part of the molecule constituted about 19, 10, and 4%, respectively (Fig. 3). Correlation of Laquinimod Metabolism toward Other Specific P450 Activities across a Panel of Human Livers. Laquinimod metabolism was determined in microsomal preparations ...
Antimicrobial peptides: an overview of a promising class
... C-terminal 37 domain of the only human cathelicidin h-CAP 18, LL-37, is an amphipathic, helical peptide that exerts broad antimicrobial activity [21]. LL-37 has been found to have additional defensive roles such as regulating the inflammatory response and chemo-attracting cells of the adaptive immune ...
... C-terminal 37 domain of the only human cathelicidin h-CAP 18, LL-37, is an amphipathic, helical peptide that exerts broad antimicrobial activity [21]. LL-37 has been found to have additional defensive roles such as regulating the inflammatory response and chemo-attracting cells of the adaptive immune ...
Elastin-like Polypeptide (ELP) Platform: Creation of Differentiated
... cardiomyopathy is the leading cause of death in DMD patients and deterioration is progressive from an early age. Evaluation of PB1046 in mdx knockout mice and mdx/utr double knockout mice demonstrated positive effects on cardiac function and skeletal muscle. VIP has also been shown to play a role in ...
... cardiomyopathy is the leading cause of death in DMD patients and deterioration is progressive from an early age. Evaluation of PB1046 in mdx knockout mice and mdx/utr double knockout mice demonstrated positive effects on cardiac function and skeletal muscle. VIP has also been shown to play a role in ...
analgesic and anti-inflammatory activity of different fractions of
... The following acute and sub acute models were selected to evaluate the anti-inflammatory activity. Carrageenan-induced rat paw edema model has been commonly used as an experimental animal model for acute inflammation and is believed to be biphasic. The early phase (1-2 h) of the carrageenan model is ...
... The following acute and sub acute models were selected to evaluate the anti-inflammatory activity. Carrageenan-induced rat paw edema model has been commonly used as an experimental animal model for acute inflammation and is believed to be biphasic. The early phase (1-2 h) of the carrageenan model is ...
(acts directly to convert plasminogen into plasmin).
... • Should be given as soon as possible. • Fibrinolytics are given intravenously. • Bleeding can occur (Systemic fibrinolysis). ...
... • Should be given as soon as possible. • Fibrinolytics are given intravenously. • Bleeding can occur (Systemic fibrinolysis). ...
Session 4 Topics Need to Monitor Aspirin Therapy
... Prasugrel (Effient®) • Theinophyridine like clopidogrel • Prodrug metabolized to active metabolite in the liver by cytochrome system • Inhibits platelet function by irreversibly binding P2Y12 ADP platelet receptors • Appears to be unaffected by cytochrome polymorphisms that inhibit clopidogrel ...
... Prasugrel (Effient®) • Theinophyridine like clopidogrel • Prodrug metabolized to active metabolite in the liver by cytochrome system • Inhibits platelet function by irreversibly binding P2Y12 ADP platelet receptors • Appears to be unaffected by cytochrome polymorphisms that inhibit clopidogrel ...
Structural Basis for Pharmacology of Voltage
... IV (Fig. 1, A and B) (Ragsdale et al., 1994, 1996; Wang et al., 1998; Yarov-Yarovoy et al., 2001, 2002). These drugs bind to a common receptor site in the pore and impede ion permeation. The amino acid residues that form the receptor sites for sodium channel blockers line the inner surface of the S6 ...
... IV (Fig. 1, A and B) (Ragsdale et al., 1994, 1996; Wang et al., 1998; Yarov-Yarovoy et al., 2001, 2002). These drugs bind to a common receptor site in the pore and impede ion permeation. The amino acid residues that form the receptor sites for sodium channel blockers line the inner surface of the S6 ...
preventing Cardiovascular Complications of hypertension
... Hypertension has reached pandemic proportions. Merely controlling the numbers of systolic & diastolic blood pressure is no longer the goal. Reducing the overall risk of the individual for cardiovascular events, preventing target organ dysfunction, yet maintaining quality of life & minimizing medicat ...
... Hypertension has reached pandemic proportions. Merely controlling the numbers of systolic & diastolic blood pressure is no longer the goal. Reducing the overall risk of the individual for cardiovascular events, preventing target organ dysfunction, yet maintaining quality of life & minimizing medicat ...
Atorvastatin
... inhibitors.[1378] Atorvastatin doses of 10—80 mg once daily result in mean LDL reductions ranging from 43—60%. Triglycerides are lowered in patients with hypertriglyceridemia by as much as 45%[1379] and HDL cholesterol increases by as much as 12% with atorvastatin monotherapy. The combination of ato ...
... inhibitors.[1378] Atorvastatin doses of 10—80 mg once daily result in mean LDL reductions ranging from 43—60%. Triglycerides are lowered in patients with hypertriglyceridemia by as much as 45%[1379] and HDL cholesterol increases by as much as 12% with atorvastatin monotherapy. The combination of ato ...
Discovery and development of ACE inhibitors
The discovery of an orally inactive peptide from snake venom established the important role of angiotensin converting enzyme (ACE) inhibitors in regulating blood pressure. This led to the development of Captopril, the first ACE inhibitor. When the adverse effects of Captopril became apparent new derivates were designed. Then after the discovery of two active sites of ACE: N-domain and C-domain, the development of domain-specific ACE inhibitors began.