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Cilostazol
Cilostazol, sold under the brand name Pletal among others, is a medication used to help the symptoms of intermittent claudication in peripheral vascular disease. If no improvement is seen after 3 months, stopping the medication is reasonable. It may also be used to prevent stroke. It is taken by mouth. Common side effects include headache, diarrhea, dizziness, and cough. Serious side effects may include decreased survival in those with heart failure, low platelets, and low white blood cells. Cilostazol is a phosphodiesterase 3 inhibitor which works by inhibiting platelet aggregation and dilating arteries. Cilostazol was approved for medical use in the United States in 1999. It is available as a generic medication. In 2019, it was the 347th most commonly prescribed medication in the United States, with more than 800thousand prescriptions. Medical uses Cilostazol is approved for the treatment of intermittent claudication in the United States and United Kingdom. Cilostazol i ...
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Peripheral Vascular Disease
Peripheral artery disease (PAD) is a vascular disorder that causes abnormal narrowing of arteries other than those that supply the heart or brain. PAD can happen in any blood vessel, but it is more common in the legs than the arms. When narrowing occurs in the heart, it is called coronary artery disease (CAD), and in the brain, it is called cerebrovascular disease. Peripheral artery disease most commonly affects the legs, but other arteries may also be involved, such as those of the arms, neck, or kidneys. Peripheral artery disease (PAD) is a form of peripheral vascular disease. Vascular refers to the arteries and veins within the body. PAD differs from peripheral veinous disease. PAD means the arteries are narrowed or blocked—the vessels that carry oxygen-rich blood as it moves from the heart to other parts of the body. Peripheral veinous disease, on the other hand, refers to problems with veins—the vessels that bring the blood back to the heart. The classic symptom is ...
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Phosphodiesterase 3 Inhibitor
A PDE3 inhibitor is a drug which inhibits the action of the phosphodiesterase enzyme PDE3. They are used for the therapy of acute heart failure and cardiogenic shock. Medical uses Cardiac Amrinone, milrinone and enoximone are used clinically for short-term treatment of cardiac failure in the presence of cardiogenic shock. PDE3 inhibitors are indicated as inotropics for the therapy of acute heart failure if catecholamines are ineffective. Well controlled studies have shown that these drugs generally increase Mortality rate, mortality, when used for the therapy of acute heart failure, so they have to be applied under close observation. Peripheral artery disease Cilostazol is used for the treatment of intermittent claudication. This drug has a much weaker positive inotropic effect than those drugs used for the therapy of acute heart failure, and lacks significant adverse cardiac effects. Contraindications Cardiac Contraindications are severe obstructive cardiomyopathy, hypo ...
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Platelet Aggregation Inhibitor
An antiplatelet drug (antiaggregant), also known as a platelet agglutination inhibitor or platelet aggregation inhibitor, is a member of a class of pharmaceuticals that decrease platelet aggregation and inhibit thrombus formation. They are effective in the arterial circulation where classical Vitamin K antagonist anticoagulants have minimal effect. Antiplatelet drugs are widely used in primary and secondary prevention of thrombotic disease, especially myocardial infarction and ischemic stroke. Antiplatelet therapy with one or more of these drugs decreases the ability of blood clots to form by interfering with the platelet activation process in primary hemostasis. Antiplatelet drugs can reversibly or irreversibly inhibit the process involved in platelet activation resulting in decreased tendency of platelets to adhere to one another and to damaged blood vessels' endothelium. Choice Antiplatelet medications are one of the primary recommendations for treatment of both stable a ...
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Intermittent Claudication
Intermittent claudication, also known as vascular claudication, is a symptom that describes muscle pain on mild exertion (ache, cramp, numbness or sense of fatigue), classically in the calf muscle, which occurs during exercise, such as walking, and is relieved by a short period of rest. It is classically associated with early-stage peripheral artery disease, and can progress to critical limb ischemia unless treated or risk factors are modified and maintained. Claudication derives . Signs and symptoms One of the hallmarks of arterial claudication is that it occurs intermittently. It disappears after a very brief rest and the patient can start walking again until the pain recurs. The following signs are general signs of atherosclerosis of the lower extremity arteries: * cyanosis * atrophic changes like loss of hair, shiny skin * decreased temperature * decreased pulse * redness when limb is returned to a "dependent" position (part of Buerger's test) The six "P"s of ischemia * Pa ...
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Cytochrome P450
Cytochromes P450 (P450s or CYPs) are a Protein superfamily, superfamily of enzymes containing heme as a cofactor (biochemistry), cofactor that mostly, but not exclusively, function as monooxygenases. However, they are not omnipresent; for example, they have not been found in ''Escherichia coli''. In mammals, these enzymes oxidize steroids, fatty acids, xenobiotics, and participate in many biosyntheses. By hydroxylation, CYP450 enzymes convert xenobiotics into hydrophilic derivatives, which are more readily excreted. P450s are, in general, the terminal oxidase enzymes in electron transfer chains, broadly categorized as P450-containing systems. The term "P450" is derived from the spectrophotometry, spectrophotometric peak at the wavelength of the absorption spectroscopy, absorption maximum of the enzyme (450 nanometre, nm) when it is in the redox, reduced state and complexed with carbon monoxide. Most P450s require a protein partner to deliver one or more electrons to reduc ...
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Tachycardia
Tachycardia, also called tachyarrhythmia, is a heart rate that exceeds the normal resting rate. In general, a resting heart rate over 100 beats per minute is accepted as tachycardia in adults. Heart rates above the resting rate may be normal (such as with exercise) or abnormal (such as with electrical problems within the heart). Complications Tachycardia can lead to fainting. When the rate of blood flow becomes too rapid, or fast blood flow passes on damaged endothelium, it increases the friction within vessels resulting in turbulence and other disturbances. According to the Virchow's triad, this is one of the three conditions (along with hypercoagulability and endothelial injury/dysfunction) that can lead to thrombosis (i.e., blood clots within vessels). Causes Some causes of tachycardia include: * Adrenergic storm * Anaemia * Anxiety * Atrial fibrillation * Atrial flutter * Atrial tachycardia * Atrioventricular reentrant tachycardia * AV nodal reentrant tachy ...
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Palpitations
Palpitations occur when a person becomes aware of their heartbeat. The heartbeat may feel hard, fast, or uneven in their chest. Symptoms include a very fast or irregular heartbeat. Palpitations are a sensory symptom. They are often described as a skipped beat, a rapid flutter, or a pounding in the chest or neck. Palpitations are not always the result of a physical problem with the heart and can be linked to anxiety. However, they may signal a arrhythmia, fast or irregular heartbeat. Palpitations can be brief or long-lasting. They can be intermittent or continuous. Other symptoms can include dizziness, shortness of breath, sweating, headaches, and chest pain. There are a variety of causes of palpitations not limited to the following: Palpitation may be associated with coronary artery disease, coronary heart disease, perimenopause, hyperthyroidism, adult heart muscle diseases like hypertrophic cardiomyopathy, congenital heart diseases like atrial septal defects, diseases causing ...
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Isoenzyme
In biochemistry, isozymes (also known as isoenzymes or more generally as multiple forms of enzymes) are enzymes that differ in amino acid sequence but catalyze the same chemical reaction. Isozymes usually have different kinetic parameters (e.g. different ''K''M values), or are regulated differently. They permit the fine-tuning of metabolism to meet the particular needs of a given tissue or developmental stage. In many cases, isozymes are encoded by homologous genes that have diverged over time. Strictly speaking, enzymes with different amino acid sequences that catalyse the same reaction are isozymes if encoded by different genes, or allozymes if encoded by different alleles of the same gene; the two terms are often used interchangeably. Introduction Isozymes were first described by R. L. Hunter and Clement Markert (1957) who defined them as ''different variants of the same enzyme having identical functions and present in the same individual''. This definition encompasses ...
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Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ...
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Enzyme Induction And Inhibition
Enzyme induction is a process in which a molecule (''e.g.'' a drug) induces (''i.e.'' initiates or enhances) the expression of an enzyme. Enzyme inhibition can refer to * the inhibition of the expression of the enzyme by another molecule * interference at the enzyme-level, basically with how the enzyme works. This can be competitive inhibition, uncompetitive inhibition, non-competitive inhibition or partially competitive inhibition. If the molecule induces enzymes that are responsible for its own metabolism, this is called auto-induction (or auto-inhibition if there is inhibition). These processes are particular forms of gene expression regulation. These terms are of particular interest to pharmacology, and more specifically to drug metabolism and drug interactions. They also apply to molecular biology. History In the late 1950s and early 1960s, the French molecular biologists François Jacob and Jacques Monod became the first to explain enzyme induction, in the context of ...
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Heat Intolerance
Heat intolerance is a symptom characterized by feeling overheated in warm environments or when the surrounding environment's temperature rises. Typically, the person feels uncomfortably hot and sweats excessively. Compared to heat illnesses like heatstroke, heat intolerance is usually a symptom of endocrine disorders, drugs, or other medical conditions, rather than the result of too much exercise or hot, humid weather. Symptoms * Feeling subjectively hot * Sweating, which may be excessive In patients with multiple sclerosis (MS), heat intolerance may cause a pseudoexacerbation, which is a temporary worsening of MS-related symptoms. A temporary worsening of symptoms can also happen in patients with postural orthostatic tachycardia syndrome (POTS) and dysautonomia. Diagnosis Diagnosis is largely made from the patient history, followed by blood tests and other medical tests to determine the underlying cause. In women, hot flashes must be excluded. Causes Excess thyroid hormone ...
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Itraconazole
Itraconazole, sometimes abbreviated ITZ, is an antifungal medication used to treat a number of fungal infections. This includes aspergillosis, blastomycosis, coccidioidomycosis, histoplasmosis, and paracoccidioidomycosis. It may be given by mouth or intravenously. Common side effects include nausea, diarrhea, abdominal pain, rash, and headache. Severe side effects may include liver problems, heart failure, Stevens–Johnson syndrome and allergic reactions including anaphylaxis. It is unclear if use during pregnancy or breastfeeding is safe. It is in the triazole family of medications. It stops fungal growth by affecting the cell membrane or affecting their metabolism. Itraconazole was patented in 1978 and approved for medical use in the United States in 1992. It is on the World Health Organization's List of Essential Medicines. Recent research works suggest itraconazole (ITZ) could also be used in the treatment of cancer by inhibiting the hedgehog pathway in a ...
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