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Guanabenz
Guanabenz (pronounced GWAHN-a-benz, sold under the trade name Wytensin) is an Alpha-adrenergic agonist, alpha agonist that is selective to the alpha-2 adrenergic receptor. Guanabenz is used as an antihypertensive drug used in the treatment of high blood pressure (hypertension). The most common side effects during guanabenz therapy are dizziness, drowsiness, dry mouth, headache and weakness. Guanabenz can make one drowsy or less alert, therefore driving or operating dangerous machinery is not recommended. Research Guanabenz also has some anti-inflammatory properties in different pathological situations, including multiple sclerosis. Guanabenz was found in one study to exert an inhibitory effect by decreasing the abundance of the enzyme CH25H, a cholesterol hydroxylase linked to antiviral immunity. Therefore, it is suggested that the drug and similar compounds could be used to treat type I interferon-dependent pathologies and that the CH25H enzyme could be a therapeutic target ...
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Alpha-adrenergic Agonist
Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The alpha-adrenergic receptor has two subclasses α1 and α2. Alpha 2 receptors are associated with sympatholytic properties. Alpha-adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with norepinephrine being the highest affinity. The activation of α1 stimulates the membrane bound enzyme phospholipase C, and activation of α2 inhibits the enzyme adenylate cyclase. Inactivation of adenylate cyclase in turn leads to the inactivation of the secondary messenger cyclic adenosine monophosphate and induces smooth muscle and blood vessel constriction. Classes Although complete selectivity between receptor agonism is rarely achieved, some agents have partial selectivity. NB: the inclusion of a drug in each ca ...
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Antihypertensive
Antihypertensives are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke, heart failure, kidney failure and myocardial infarction. Evidence suggests that a reduction of blood pressure by 5 mmHg can decrease the risk of stroke by 34% and of ischaemic heart disease by 21%. It can reduce the likelihood of dementia, heart failure, and mortality from cardiovascular disease. There are many classes of antihypertensives, which lower blood pressure by different means. Among the most important and most widely used medications are thiazide diuretics, calcium channel blockers, angiotensin-converting enzyme inhibitors (ACE inhibitors), angiotensin II receptor blockers or antagonists (ARBs), and beta blockers. Which type of medication to use initially for hypertension has been the subject of several large studies and resulting national guidelines. The fundamental ...
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Guanfacine
Guanfacine, sold under the brand name Tenex ( immediate-release) and Intuniv ( extended-release) among others, is an oral alpha-2a agonist medication used to treat attention deficit hyperactivity disorder (ADHD) and high blood pressure. Common side effects include sleepiness, constipation, and dry mouth. Other side effects may include low blood pressure and urinary problems. It appears to work by activating α2A-adrenergic receptors in the brain, thereby decreasing sympathetic nervous system activity. Guanfacine was first described in 1974 and was approved for medical use in the United States in 1986. It is available as a generic medication. In 2022, it was the 275th most commonly prescribed medication in the United States, with more than 800,000 prescriptions. Guanfacine is approved by the US FDA for monotherapy treatment of ADHD, as well as being used for augmentation of stimulant medications. Guanfacine is also used off-label to treat tic disorders, anxiety disor ...
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Alpha-2 Adrenergic Receptor Agonists
Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The alpha-adrenergic receptor has two subclasses α1 and α2. Alpha 2 receptors are associated with sympatholytic properties. Alpha-adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with norepinephrine being the highest affinity. The activation of α1 stimulates the membrane bound enzyme phospholipase C, and activation of α2 inhibits the enzyme adenylate cyclase. Inactivation of adenylate cyclase in turn leads to the inactivation of the secondary messenger cyclic adenosine monophosphate and induces smooth muscle and blood vessel constriction. Classes Although complete selectivity between receptor agonism is rarely achieved, some agents have partial selectivity. NB: the inclusion of a drug in each cat ...
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Alpha-2 Adrenergic Receptor
The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi alpha subunit, Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-adrenergic, α2A-, α2B-adrenergic, α2B-, and α2C-adrenergic, α2C-adrenergic. Some species other than humans express a fourth α2D-adrenergic receptor as well. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α2-adrenergic receptor in the central nervous system, central and peripheral nervous systems. Cellular localization The Alpha-2A adrenergic receptor, α2A adrenergic receptor is localised in the following central nervous system (CNS) structures: * Brainstem (especially the locus coeruleus as presynaptic & somatodendritic autoreceptor ) * Midbrain * Hypothalamus * Olfactory system * Hippocampus * Spinal cord * Cerebral cortex * Cerebellum * Septum Whereas the Alpha-2B adrenergic receptor, α2B adren ...
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Hypertension
Hypertension, also known as high blood pressure, is a Chronic condition, long-term Disease, medical condition in which the blood pressure in the artery, arteries is persistently elevated. High blood pressure usually does not cause symptoms itself. It is, however, a major risk factor for stroke, coronary artery disease, heart failure, atrial fibrillation, peripheral arterial disease, vision loss, chronic kidney disease, and dementia. Hypertension is a major cause of premature death worldwide. High blood pressure is classified as essential hypertension, primary (essential) hypertension or secondary hypertension. About 90–95% of cases are primary, defined as high blood pressure due to non-specific lifestyle and Genetics, genetic factors. Lifestyle factors that increase the risk include excess salt in the diet, overweight, excess body weight, smoking, physical inactivity and Alcohol (drug), alcohol use. The remaining 5–10% of cases are categorized as secondary hypertension, d ...
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Dizziness
Dizziness is an imprecise term that can refer to a sense of disorientation in space, vertigo, or lightheadedness. It can also refer to Balance disorder, disequilibrium or a non-specific feeling, such as giddiness or foolishness. Dizziness is a common medical complaint, affecting 20–30% of persons. Dizziness is broken down into four main subtypes: vertigo (~25–50%), equilibrioception#Dysfunction, disequilibrium (less than ~15%), presyncope (less than ~15%), and nonspecific dizziness (~10%). * Vertigo is the sensation of spinning or having one's surroundings spin about them. Many people find vertigo very disturbing and often report associated nausea and vomiting. * Presyncope describes lightheadedness or feeling faint; the name relates to Syncope (medicine), syncope, which is actually fainting. * equilibrioception#Dysfunction, Disequilibrium is the sensation of being off balance and is most often characterized by frequent falls in a specific direction. This condition is not of ...
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Drowsiness
Somnolence (alternatively sleepiness or drowsiness) is a state of strong desire for sleep, or sleeping for unusually long periods (compare hypersomnia). It has distinct meanings and causes. It can refer to the usual state preceding falling asleep, the condition of being in a drowsy state due to circadian rhythm disorders, or a symptom of other health problems. It can be accompanied by lethargy, weakness and lack of mental agility. Somnolence is often viewed as a symptom rather than a disorder by itself. However, the concept of somnolence recurring at certain times for certain reasons constitutes various disorders, such as excessive daytime sleepiness, shift work sleep disorder, and others; and there are medical codes for somnolence as viewed as a disorder. Sleepiness can be dangerous when performing tasks that require constant concentration, such as driving a vehicle. When a person is sufficiently fatigued, microsleeps may be experienced. In individuals deprived of sleep, som ...
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Dry Mouth
Xerostomia, also known as dry mouth, is a subjective complaint of dryness in the mouth, which may be associated with a change in the composition of saliva, reduced salivary flow, or have no identifiable cause. This symptom is very common and is often seen as a side effect of many types of medication. It is more common in older people (mostly because individuals in this group are more likely to take several medications) and in people who breathe through their mouths. Dehydration, radiotherapy involving the salivary glands, chemotherapy and several diseases can cause reduced salivation (hyposalivation), or a change in saliva consistency and hence a complaint of xerostomia. Sometimes there is no identifiable cause, and there may sometimes be a psychogenic reason for the complaint. Definition Xerostomia is the subjective sensation of dry mouth, which is often (but not always) associated with hypofunction of the salivary glands. The term is derived from the Greek words ξηρός (' ...
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Headache
A headache, also known as cephalalgia, is the symptom of pain in the face, head, or neck. It can occur as a migraine, tension-type headache, or cluster headache. There is an increased risk of Depression (mood), depression in those with severe headaches. Headaches can occur as a result of many conditions. There are a number of different classification systems for headaches. The most well-recognized is that of the International Headache Society, which classifies it into more than 150 types of Primary headache disorder, primary and secondary headaches. Causes of headaches may include dehydration; fatigue; sleep deprivation; Stress (biology), stress; the effects of medications (overuse) and recreational drugs, including withdrawal; viral infections; loud noises; head injury; rapid ingestion of a very cold food or beverage; and dental or sinus issues (such as sinusitis). Treatment of a headache depends on the underlying cause, but commonly involves analgesic, pain medication (esp ...
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Weakness
Weakness is a symptom of many different medical conditions. The causes are many and can be divided into conditions that have true or perceived muscle weakness. True muscle weakness is a primary symptom of a variety of skeletal muscle diseases, including muscular dystrophy and inflammatory myopathy. It occurs in neuromuscular junction disorders, such as myasthenia gravis. Pathophysiology Muscle cells work by detecting a flow of electrical impulses from the brain, which signals them to contract through the release of calcium by the sarcoplasmic reticulum. Fatigue (reduced ability to generate force) may occur due to the nerve, or within the muscle cells themselves. New research from scientists at Columbia University suggests that muscle fatigue is caused by calcium leaking out of the muscle cell. This makes less calcium available for the muscle cell. In addition, the Columbia researchers propose that an enzyme activated by this released calcium eats away at muscle fibers. Su ...
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