Antihypotensive Agents
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Antihypotensive Agents
An antihypotensive, also known as a vasopressor, is an agent that raises blood pressure by constricting blood vessels, thereby increasing systemic vascular resistance. This is different from inotropes which increase the force of cardiac contraction. Some substances do both (e.g. dopamine, dobutamine). If low blood pressure is due to blood loss, then preparations increasing volume of blood circulation—plasma-substituting solutions such as colloid and crystalloid solutions (salt solutions)—will raise the blood pressure without any direct vasopressor activity. Packed red blood cells, plasma or whole blood should not be used solely for volume expansion or to increase oncotic pressure of circulating blood. Blood products should only be used if reduced oxygen carrying capacity or coagulopathy is present. Other causes of either absolute (dehydration, loss of plasma via wound/burns) or relative ( third space losses) vascular volume depletion also respond, although blood products are ...
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Blood Pressure
Blood pressure (BP) is the pressure of Circulatory system, circulating blood against the walls of blood vessels. Most of this pressure results from the heart pumping blood through the circulatory system. When used without qualification, the term "blood pressure" refers to the pressure in a brachial artery, where it is most commonly measured. Blood pressure is usually expressed in terms of the systolic pressure (maximum pressure during one Cardiac cycle, heartbeat) over diastolic pressure (minimum pressure between two heartbeats) in the cardiac cycle. It is measured in Millimetre of mercury, millimetres of mercury (mmHg) above the surrounding atmospheric pressure, or in Pascal (unit), kilopascals (kPa). The difference between the systolic and diastolic pressures is known as pulse pressure, while the average pressure during a cardiac cycle is known as mean arterial pressure. Blood pressure is one of the vital signs—together with respiratory rate, heart rate, Oxygen saturation (me ...
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Dobutamine
Dobutamine is a medication used in the treatment of cardiogenic shock (as a result of inadequate tissue perfusion) and severe heart failure. It may also be used in certain types of cardiac stress tests. It is given by IV only, as an injection into a vein or intraosseous as a continuous infusion. The amount of medication needs to be adjusted to the desired effect. Onset of effects is generally seen within 2 minutes. It has a half-life of two minutes. This drug is generally only administered short term, although it may be used for longer periods to relieve symptoms of heart failure in patients awaiting heart transplantation. Common side effects include a fast heart rate, an irregular heart beat, and inflammation at the site of injection. Use is not recommended in those with idiopathic hypertrophic subaortic stenosis. It primarily works by direct stimulation of β1 receptors, which increases the strength of the heart's contractions, leading to a positive inotropic effect. ...
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Hydrocortisone
Hydrocortisone is the name for the hormone cortisol when supplied as a medication. It is a corticosteroid and works as an anti-inflammatory and by immune suppression. Uses include conditions such as adrenocortical insufficiency, adrenogenital syndrome, high blood calcium, thyroiditis, rheumatoid arthritis, dermatitis, asthma, and COPD. It is the treatment of choice for adrenocortical insufficiency. It can be given by mouth, topically, rectally or by injection. Stopping treatment after long-term use should be done slowly. Common side effects may include mood changes, increased appetite, hyperglycemia, hypertension, and edema (swelling). With long-term use, common side effects include osteoporosis, adrenal insufficiency, upset stomach, physical weakness, easy bruising, and candidiasis (yeast infections). It is unclear if it is safe for use during pregnancy. Hydrocortisone was patented in 1936 and approved for medical use in 1941. It is on the World Health Orga ...
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Mineralocorticoids
Mineralocorticoids are a class of corticosteroids, which in turn are a class of steroid hormones. Mineralocorticoids are produced in the adrenal cortex and influence salt and water balances (electrolyte balance and fluid balance). The primary mineralocorticoid is aldosterone. Physiology The name mineralocorticoid derives from early observations that these hormones were involved in the retention of sodium, a mineral. The primary endogenous mineralocorticoid is aldosterone, although a number of other endogenous hormones (including progesterone and deoxycorticosterone) have mineralocorticoid function. Aldosterone acts on the kidneys to provide active reabsorption of sodium and an associated passive reabsorption of water, as well as the active secretion of potassium in the principal cells of the cortical collecting tubule and active secretion of protons via proton ATPases in the lumenal membrane of the intercalated cells of the collecting tubule. This in turn results in an incre ...
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Glucocorticoids
Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebrate animal cell. The name "glucocorticoid" is a portmanteau of "glucose", "cortex", and "steroid" and is composed from its role in regulation of glucose metabolism, synthesis in the adrenal cortex, and its steroidal structure (see structure below). Glucocorticoids are part of the feedback mechanism in the immune system, which reduces certain aspects of immune function, such as inflammation. They are therefore used in medicine to treat diseases caused by an overactive immune system, such as allergies, asthma, autoimmune diseases, and sepsis. Glucocorticoids have many diverse effects such as pleiotropy, including potentially harmful side effects. They also interfere with some of the abnormal mechanisms in cancer cells, so they are used in ...
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Difetur
''S''-Ethylisothiouronium diethylphosphate (brand name Difetur) is an ''S''-alkylisothiouronium derivative used as an antihypotensive drug. The ''S''-alkylisothiouronium compounds are used in processes of treating acute hypotension, which may result, for example, from shock or hemorrhage, and in processes for treating hyperoxic conditions, for example, oxygen poisoning. Indications It is used for increasing arterial blood pressure in cases of acute arterial hypotension due to surgical interference, trauma, poisoning, shock condition, hemorrhages; in conjunction with epidural anesthesia; in overdose of ganglion blockers, alpha-adrenergic blockers, neuroleptics, anesthetics; and in other conditions when adrenomimetics are contra-indicated or ineffective. Difetur was also found to possess oxygen protective activity and, thus, can be used as a medicament for protecting against oxygen poisoning conditions caused by hyperoxia. ''S''-Ethylisothiouronium diethylphosphate is also used f ...
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Angiotensinamide
Angiotensinamide ( INN; BAN and USAN angiotensin amide) is a potent vasoconstrictor used as a cardiac stimulant. It is a derivative of angiotensin II. See also * Angiotensin Angiotensin is a peptide hormone that causes vasoconstriction and an increase in blood pressure. It is part of the renin–angiotensin system, which regulates blood pressure. Angiotensin also stimulates the release of aldosterone from the adr ... References {{Cardiac stimulants excluding cardiac glycosides Antihypotensive agents Cardiac stimulants ...
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Vasopressin
Mammalian vasopressin, also called antidiuretic hormone (ADH), arginine vasopressin (AVP) or argipressin, is a hormone synthesized from the ''AVP'' gene as a peptide prohormone in neurons in the hypothalamus, and is converted to AVP. It then travels down the axon terminating in the posterior pituitary, and is released from vesicles into the circulation in response to extracellular fluid hypertonicity ( hyperosmolality). AVP has two primary functions. First, it increases the amount of solute-free water reabsorbed back into the circulation from the filtrate in the kidney tubules of the nephrons. Second, AVP constricts arterioles, which increases peripheral vascular resistance and raises arterial blood pressure. A third function is possible. Some AVP may be released directly into the brain from the hypothalamus, and may play an important role in social behavior, sexual motivation and pair bonding, and maternal responses to stress. Vasopressin induces differentiation o ...
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Metaraminol
Metaraminol, also known as metaradrine and sold under the brand name Aramine among others, is a sympathomimetic medication which is used in the prevention and treatment of hypotension (low blood pressure), particularly as a complication of anesthesia. It is given by intramuscular or intravenous administration. Side effects of metaraminol include reflex bradycardia among others. Metaraminol is a norepinephrine releasing agent and at high doses a α1-adrenergic receptor agonist with some β-adrenergic effect. It is a substituted amphetamine and is closely related to phenylpropanolamine, ephedrine, and oxilofrine. Metaraminol was approved for medical use in the United States in September 1954. Medical uses Metaraminol is given intravenously as either a bolus (often 0.5–1 mg doses) or as an infusion, usually via peripheral intravenous access. Metaraminol is commonly available as 10 mg in 1 mL, that requires dilution prior to administration (often made ...
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Amezinium
Amezinium metilsulfate (INN, trade name Regulton) is a sympathomimetic drug used for the treatment of low blood pressure. It has multiple mechanisms, including stimulation of alpha and beta-1 receptors and inhibition of noradrenaline and tyramine Tyramine ( ) (also spelled tyramin), also known under several other names, is a naturally occurring trace amine derived from the amino acid tyrosine. Tyramine acts as a catecholamine releasing agent. Notably, it is unable to cross the bl ... uptake. Synthesis This antidepressant is made from Chloridazon starting material. The halogenation of 2-Butyne-1,4-diol 10-65-6(1) with chlorine gives Mucochloric acid 7-56-9(2). Treatment with Phenylhydrazine 00-63-0(3) gives 1-Phenyl-4,5-dichloro-6-pyridazone 698-53-9(4). Addition of ammonia leads to Chloridazon 698-60-8(5). Catalytic hydrogenation yields 5-amino-2-phenylpyridazin-3-one 3589-77-0(6). Alkylation with dimethyl sulfate completed the synthesis of Amezinium metisulf ...
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Midodrine
Midodrine, sold under the brand names ProAmatine and Orvaten among others, is an antihypotensive medication used to treat orthostatic hypotension (low blood pressure when standing) and urinary incontinence. It is taken oral administration, by mouth. Side effects of midodrine include hypertension (high blood pressure), paresthesia, pruritus, itching, goosebumps, chills, urinary urgency, urinary retention, and urinary frequency. Midodrine is a prodrug of its active metabolite desglymidodrine. This metabolite acts as a binding selectivity, selective agonist of the alpha-1 adrenergic receptor, α1-adrenergic receptor. This in turn results in vasoconstriction and increased blood pressure. Midodrine was discovered by 1971 and was introduced for medical use in the United States in 1996. Medical uses Midodrine is indicated for the treatment of symptomatic orthostatic hypotension. It can reduce dizziness and faints by about a third, but can be limited by troublesome goose bumps, prur ...
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