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Selective phosphodiesterase inhibitors for the treatment
Selective phosphodiesterase inhibitors for the treatment

... inhibitors such as opsonized zymosan-stimulated superoxide generation [70,71], platelet-activating factor (PAF)- and C5a-induced LTC4 production, as well as chemotaxis [25,72]. Furthermore, in the presence of a b-adrenoceptor agonist, PDE4 inhibitors reduced the release of eosinophil cationic protei ...
Complete Steroid Avoidance Is Effective and Safe in Children With
Complete Steroid Avoidance Is Effective and Safe in Children With

... immunosuppressive agents are given in large doses . However, such a strategy could induce a state of overimmunosuppression with an increased risk of such complications as posttransplant lymphoproliferative disorder . A steroid-free (SF) protocol for pediatric kidney transplant recipients was develop ...
The Safety of COX
The Safety of COX

... new drug application. Such an application would be reviewed with consideration of the risk to benefit balance of the proposed indications and populations for use, warnings in the label, and all relevant data. We expect that the proposal would also be reviewed at a public Advisory Committee meeting. ...
Aripiprazole LAI Prescribing Guidelines
Aripiprazole LAI Prescribing Guidelines

... of schizophrenia in adult patients stabilised with oral aripiprazole. 2. Aripiprazole LAI may not be used for treatment-resistant schizophrenia, unlicensed indications or service users intolerant to or unresponsive oral aripiprazole. 3. Aripiprazole LAI may ONLY be newly prescribed by consultant psy ...
Review article: prevention of non-steroidal anti
Review article: prevention of non-steroidal anti

... H2 -receptor antagonists In a pooled analysis of five randomized-controlled trials of H2 -receptor antagonists for the prevention of gastroduodenal ulcers associated with NSAID use, it was found that standard doses of H2 -receptor antagonists reduced the risk of duodenal but not gastric ulcers.17 Da ...
Effect of Hepatic Dysfunction on Oral Cyclosporine
Effect of Hepatic Dysfunction on Oral Cyclosporine

... at therapeutic concentrations,2 which is important in marrow transplant patients. In patients with acute nonlymphocytic leukemia, a randomized comparison methotrexate shows that ...
Bioinformatics (2011) 27
Bioinformatics (2011) 27

... pocket represented by Ala291 and Leu219/238, respectively. The enclosure of the guest molecules within the pocket is driven by formation of multiple hydrophobic contacts with nonpolar site residues. On the other hand, acidic or electronegative peripherial groups of the ligands are oriented in the su ...
Therapeutic Agents for Alzheimer`s Disease
Therapeutic Agents for Alzheimer`s Disease

... blocking cholinergic neurotransmission produces some improvement or impairment in learning and memory. ACh, a neurotransmitter in the brain plays a critical role in the function of learning and memory. ACh is synthesized from acetyl-CoA and choline by cholineacetyltransferase, and is released into t ...
Prescribing guidelines for NSAIDs (including
Prescribing guidelines for NSAIDs (including

... Thrombotic risk is slightly increased with COX-II inhibitors and diclofenac (especially at doses of 150mg daily). This small increased risk is shared with ibuprofen at doses above 1200mg daily. Low dose ibuprofen – less than 1200mg daily and Naproxen up to 1000mg daily have a minimal risk. Whilst th ...
Prodrugs: Effective Solutions for Solubility, Permeability and
Prodrugs: Effective Solutions for Solubility, Permeability and

... lipophilicity. Prodrugs of simple alkyl esters, cyclic carbonate esters and acyclic double esters offer certain advantages and disadvantages. Simple alkyl esters are not usually substrates of human blood esterases, tend to rely on hepatic hydrolysis and have been used successfully for many ACE inhib ...
Equivalent dose ratios for opioids Oral morphine
Equivalent dose ratios for opioids Oral morphine

... A rough guide is the dose of diamorphine (in mg over 24 hours) is in the region of the dose of fentanyl (in micrograms per hour) Injectable diamorphine : injectable alfentanil ...
ZUCLOPENTHIXOL tab, drops , amp: Class: Typical antipsychotic
ZUCLOPENTHIXOL tab, drops , amp: Class: Typical antipsychotic

... -Long-term management of psychosis: Zuclopenthixol decanoate: I.M.: Maintenance therapy: Usual maintenance dose: 150-300 mg every 2-4 weeks; dose increase or reduction and/or more frequent administration may be required in some patients. Maintain lowest effective dose. **Transfer of patients from or ...
Matrix metalloproteinase inhibitors in rheumatic diseases
Matrix metalloproteinase inhibitors in rheumatic diseases

... specifically targeting enzymes such as the collagenases that seem to facilitate the key irreversible step to joint destruction? Both approaches have been used, although despite the variety of inhibitors so far produced, very few of these drugs have progressed into the clinic or to a stage at which t ...
Akamin
Akamin

... Anticoagulant Therapy. Patients who are on anticoagulant therapy may require downward adjustment of their anticoagulant dosage, because tetracyclines have been shown to depress plasma prothrombin activity. In long-term therapy, periodic laboratory evaluation of organ systems, including haematopoieti ...
Semprex®-D Capsules(acrivastine and pseudoephedrine
Semprex®-D Capsules(acrivastine and pseudoephedrine

... maximum plasma acrivastine concentrations were achieved at 1.14 ± 0.23 hour. A mass balance study in 7 healthy volunteers showed that acrivastine is primarily eliminated by the kidneys. Over a 72-hour collection period, about 84% of the administered total radioactivity was recovered in urine and abo ...
Data Sheet
Data Sheet

... inhibition of CYP2D6 would result in the change of phenotype into poor metabolizer (phenocopying, see Clinical pharmacology pharmacokinetic). Caution should therefore be exercised when co-administering potent CYP2D6 inhibitors with metoprolol. Known clinically significant potent inhibitors of CYP2D6 ...
Variability in CYP2C9 allele frequency
Variability in CYP2C9 allele frequency

... Background: Wide variability exists in the frequency of pharmacogenetic markers for anticoagulant response in different populations. There is insufficient data on the prevalence of these variant genotypes in the Indian population. This study aims to determine the frequency of various genotype combin ...
9-Methyl-7-Bromoeudistomin D, a Caffeine Like
9-Methyl-7-Bromoeudistomin D, a Caffeine Like

... markedly inhibited by addition of caffeine (3 mM). Furthermore, 3H-MBED binding to liver microsomes from β-NF-treated rats was concentration-dependently inhibited by α-NF (IC≒10 nM), but not by SKF525A (fig.4). In contrast, SKF525A caused an inhibition of ...
COX-2-selective NSAIDs: New wonder drugs?
COX-2-selective NSAIDs: New wonder drugs?

... secondary to their inhibition of the enzyme cyclooxygenase (COX). This results in suppression of inflammation, and effective analgesia. Most NSAIDs not only inhibit PGs at sites of inflammation, but also PGs which serve important functions in other parts of the body, a factor which accounts for some ...
Diamide, Capsule
Diamide, Capsule

... Consideration should always be given with new drugs as to possible interaction with monoamine oxidase inhibitors. Theoretically, the combination of loperamide with monoamine oxidase inhibitors, which are also inhibitors of liver microsomal enzymes, may potentiate the action of Ioperamide by blocking ...
A Review of Sodium Glucose Co transporter 2 (SGLT2)
A Review of Sodium Glucose Co transporter 2 (SGLT2)

... All of the SGLT2 inhibitors are available as an oral tablet formulation. The oral bioavailability of the SGLT2 inhibitors range from 60-78% and achieves maximum concentration 1-2 hours after administration. The elimination half-life of this class of medication ranges from 10.2-13.1 hours and have a ...
Angiotensin Converting Enzyme Inhibitors
Angiotensin Converting Enzyme Inhibitors

... Captopril contains a modified proline molecule with a mercapto moiety that binds with the zinc atom of the metalloenzyme ACE, thus inactivating it. It is easily absorbed by mouth in the active form, provided it is taken on an empty stomach (because food has been reported to diminish its bioavailabil ...
brufen sustained release (sr)
brufen sustained release (sr)

... or duration of use, but can occur at any time without warning. Upper GI ulcers, gross bleeding or perforation caused by NSAIDs occur in approximately 1% of patients treated for 3-6 months and in about 2-4% of patients treated for one year. These trends continue with longer duration of use, increasin ...
Beta blocker sotalol metoprolol conversion calculator
Beta blocker sotalol metoprolol conversion calculator

... Timolol Brevibloc Esmolol Cartrol Carteolol Up-to date list of blood pressure lowering medications by classes, including diuretics, ACE inhibitors, Beta-Blockers, Calcium Channel Blockers, Vasodilators, anti. I have been experiencing palpitations for 18 months now and am exhausted from them. I have ...
Ticagrelor — Is There Need for a New Player in the Antiplatelet
Ticagrelor — Is There Need for a New Player in the Antiplatelet

... The thienopyridine clopidogrel, which irreversibly blocks the adenosine diphosphate (ADP) receptor P2Y12 on platelets, has become an essential component of therapy in patients with acute coronary syndromes, because it significantly improves the outcomes.1 However, clopidogrel has at least three draw ...
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Discovery and development of direct thrombin inhibitors



Direct thrombin inhibitors (DTIs) are a class of anticoagulant drugs that can be used to prevent and treat embolisms and blood clots caused by various diseases. They inhibit thrombin, a serine protease which affects the coagulation cascade in many ways. DTIs have undergone rapid development since the 90's. With technological advances in genetic engineering the production of recombinant hirudin was made possible which opened the door to this new group of drugs. Before the use of DTIs the therapy and prophylaxis for anticoagulation had stayed the same for over 50 years with the use of heparin derivatives and warfarin which have some well known disadvantages. DTIs are still under development, but the research focus has shifted towards factor Xa inhibitors, or even dual thrombin and fXa inhibitors that have a broader mechanism of action by both inhibiting factor IIa (thrombin) and Xa. A recent review of patents and literature on thrombin inhibitors has demonstrated that the development of allosteric and multi-mechanism inhibitors might lead the way to a more safer anticoagulant.
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