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Tolbutamide is one of the most widely used antidiabetic agents. Its action is preferably connected with stimulatory action of -cells in the pancreas, which results in intensive insulin secretion. It is used for type II diabetes mellitus of medium severity with no expressed microvascular complications. Synonyms of this drug are mebenol, oramid, ora-bet, tolbuton, butamide, rastinon, and others. Chlorpropamide Chlorpropamide, 1-(p-chlorophenylsulfonyl)-3-propylurea (26.2.3), is made in a...

Male Sex Hormones and Anabolic Steroids

The term androgens includes a number of natural and synthetic compounds that exhibit the masculinizing and anabolic action of testosterone, the main physiological, endogenic, and androgenic hormone. Androgens, commonly referred to as male sex hormones or anabolic steroids, in particular, testosterone, are produced by male sex glands in the male body. Androgens have masculinizing, anabolic, and growth-stimulating effects. They are responsible for the development of sex organs, secondary sex...

Anthranylic acid derivatives

Anthranylic acid derivatives are direct structural analogs of salicylic acid derivatives. They possess analgesic, anti-inflammatory, and fever-reducing activity. They are similar to pyrazolones in terms of analgesic and fever-reducing activity, yet they exceed the antiinflammatory activity of salicylates. The mechanism of action of this series of nonsteroid, anti-inflammatory analgesics is not conclusively known. Flufenamic acid Flufenamic acid, N-(a,a,a-trifluoro-m-tolyl)anthranylic acid...

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H2 pd-c ) )n, -ch30 ch2 nh2 Trimethoprim has a broad spectrum of antimicrobial activity. It is 20-100 times more active than sulfamethoxazole with respect to most bacterial forms. Trimethoprim is active with respect to Gram-positive, aerobic bacteria such as Staphylococcus aureus, Staphylococcus epidermidis, and various types of Streptococcus and Listeria monocyto-genes. Trimethoprim is inferior to sulfonamides against forms of Nocardia. It is active with respect to Gram-negative, aerobic...

Pyrazolonees

In medicine, pyrazolonee derivatives play a significant role as analgesics, anti-inflammatory, and fever-reducing agents. Among these are antipyrin, butadion, amidopyrin, phenylpyrazon, sulfinpyrazone, sodium methamizol sodium (analgin), and a few others. In terms of analgesic and anti-inflammatory action, they are similar to salicylic acid derivatives. Although the mechanism of their action is not completely known, it is supposed that pyrazolone derivatives, like aspirin, inhibit biosynthesis...

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Atropine is used for stomach ulcers, pylorospasms, cholesystis, kidney stones, spasms of the bowels and urinary tract, and bronchial asthma. Atropine is frequently used during anesthesia in surgery. The main goal is to minimize secretion in the bronchi and nasopharynx, which can impede respiration. In cases where additional sedative action is needed, scopolamine is preferred. In ophthalmological practice, atropine is used for diagnostic purposes, dilating pupils, for severe inflammatory...

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Hexocyclium inhibits muscarinic action of acetylcholine on postganglionic parasympathetic effector regions. It is used for treating stomach ulcers. A synonym of this drug is tral. 14.1.3 Antiparkinsonian drugs of the quaternary amine series Drugs that exhibit central anticholinergic properties are used in treating Parkinsonism. It is believed that they do not affect the synthesis, release, or hydrolysis of acetylcholine. Their medicinal efficacy is manifest by the reduction or removal of motor...

Local Anesthetics

Local anesthetics are medications used for the purpose of temporary and reversible elimination of painful feelings in specific areas of the body by blocking transmission of nerve fiber impulses. Local anesthesia is any technique to render part of the body insensitive to pain without affecting consciousness. In clinical situations, local anesthetics are used in many different ways and in various situations requiring local pain relief, beginning with simple procedures such as removing a small...

Drugs Affecting The Dopaminergic Systems Of The Brain

In medical practice, four types of dopaminergic drugs are used, and they can be characterized as dopamine precursors (levodopa), dopamine-releasing drugs (amantadine), dopamine receptor agonists (bromocriptine), and dopamine inactivation inhibitors (selegiline). Dopamine precursors elevate the concentration of dopamine. Another group, dopamine-releasing drugs, was discovered accidentally while making the antiviral drug amantadine. It can be beneficial to patients who have a depot of dopamine....

Drugs stimulating predominantly aadrenoreceptors

The direct-acting adrenomimetics described next are a-adrenergic agonists that are structurally very different from the drugs described above. Clonidine Clonidine, 2-(2,6-dichlorophenylamino)imidazoline (11.1.34), is synthesized from 2,6-dichloroaniline, the reaction of which with ammonium thiocyante gives N-(2,6-dichlorophenyl)thiourea (11.1.32). Methylation of this product into (11.1.33) by the subsequent reaction with ethylendiamine gives clonidine (11.1.34) 34-39 . Clonidine is a selective...

Appetite Suppressants Or Anorectics

A group of drugs structurally related to amphetamines that suppress appetite and which are used in treatment of obesity are called analeptics. Compounds of this group exhibit a range of pharmacological and toxicological action analog to that of amphetamines, and are used as adjuvant drugs in the treatment of obe-sity,which is accomplished through an individually structured program of limiting caloric intake. Not one of the substances used exceeds amphetamines in terms of activity however, the...

Illnesses

Respiratory system diseases can originate as a result of infection, foreign agents of various natures including dust, chemical substances, and smoking aging, genetic factors, severe injury, or as a result of a hypersensitive reaction. Therapy of respiratory system illnesses generally consists of restoring appropriate physiological functions. In particular, antibiotics remove infections that have invaded the respiratory tract, glucocorticoids relieve inflammation, bronchodilators (broncholytics)...

Benzodiazepines

Before the introduction of the class of benzodiazepines, the primary drugs used for correcting psychoemotional disorders were sedative and hypnotic drugs, in particular phenobarbital and glutethimide. Benzodiazepines turned out to be extremely effective drugs for treating neurotic conditions. The first representative of this large group of compounds, chlordiazepoxide, was synthesized in the 1930s and introduced into medical practice at the end of the 1950s. More than 10 other benzodiazepine...

Anxiolytics Tranquilizers

Many illnesses are accompanied by anxiety, a worried state during which a syndrome characterized by feelings of helplessness, despair, dark premonitions, and asthenia begins to develop. It can be accompanied by headaches, increased perspiration, nausea, tachycardia, dry mouth, etc. A state of anxiety can originate from neurological reasons, and can also be of a somatopsychic nature, which is associated with pathological development in diseases of the cardiovascular system, neoplasms,...

Tricyclic Antidepressants

The most frequently used drugs are tricyclic antidepressants, which received their name from the organization of their chemical structures, in particular the systems consisting of two benzene rings joined to a central 7-membered ring with a dialkylaminoalkyl group connected to the central ring. Depending on the substituents on the terminal nitrogen atom in the amine-containing side chain, they in turn are subdivided into tertiary (imipramine, amitriptyline, trimipramine, doxepin) and secondary...

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As was already stated, erythromycin and other antibiotics discussed in this chapter inhibit the synthesis of bacterial proteins. Erythromycin inhibits bacterial protein synthesis by reversibly binding with their 50 S ribosomal subunit, thus blocking the formation of new peptide bonds. Erythromycin is classified as a bacteriostatic antibiotic. However, it can also exhibit a bactericidal effect against a few types of microbes at certain concentrations. Bacterial resistance to erythromycin can...

Insulin

Insulin, a pancreatic hormone, is a specific antidiabetic agent, especially for type I diabetes. Human insulin is a double-chain protein with molecular mass around 6000 that contains 51 amino acids (chain A 21 amino acids, chain B 30 amino acids), which are bound together by disulfide bridges. Pig insulin differs from human insulin only in that it has a different amino acid at position 30, and bovine insulin has different amino acids at positions 8,10, and 30. Insulin was discovered in 1921. It...

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Methyldopa is an a-methoxylated derivative of levodopa that exhibits hypotensive action by reducing overall peripheral vascular resistance and reducing heart work. Antihypertensive action of methyldopa consists of the biotransformation of methyldopa into methylnoradrenaline (methylnorepinephrine), which acts as a pseudo neurotransmitter. The current, universally accepted point of view is that the action of methyldopa is carried out through the CNS, where methylnorepinephrine, a powerful...

Thyroid Hormone and Antithyroid Drugs

Endogenous iodine-containing thyroid hormones L-thyroxine and L-triiodothyronine are produced by the thyroid gland, which exhibits pronounced metabolic control over practically every cell in the body using the two mentioned iodine-containing hormones. By controlling the rate of oxidative cellular processes, these hormones take part in regulation of growth and development of the organism, formation of bone marrow and bone tissue they affect activity of the CNS, cardiovascular system,...

Androgens

In applied medicine, testosterone esters (propionate, cypionate, and enantate) and a synthetic analog, methyltestosterone, are widely used. In many tissues, testosterone's androgenic effect depends on the degree to which it is turned into dihydrotestosterone by the enzyme 5-a-reductase in the target tissues. It is believed that all steroids, including testosterone, exhibit their effect by binding with corresponding receptors in target tissues. It has been shown that the affinity to androgenic...

Nonsteroid Antiinflammatory Drugs And Antifever Analgesics

A huge quantity of drugs belonging to various classes of compounds exhibit analgesic, anti-fever, and anti-inflammatory action. In addition, they are devoid of many undesirable effects that accompany opioid analgesics (respiratory depression, addiction, etc.). They are called nonnarcotic analgesics, aspirin-like substances, anti-fever analgesics, etc., in order to differentiate nonsteroidal, anti-inflammatory, and anti-fever analgesics from opioids and glucocorticoids. The exact mechanism of...

Antifungal Drugs

In comparison with bacteria or viruses, fungi are more complex organisms. They have ribosomes, cellular membrane components, and a nuclear membrane. Therefore, antibacterial antibiotics are, as a rule, ineffective against pathogenic fungi. Fungal infections (mycoses) occur less than bacterial or viral infections. However, that statement may be untrue for a few geographical regions that are favorable for the existence and growth of specific fungal pathogens. A few fungal infections can spread to...

Soporific Agents Hypnotics and Sedative Drugs

Insomnia is a symptom, and its proper treatment depends on finding the cause of sleeplessness and treating the underlying etiology. The most common type of insomnia is transient insomnia due to acute situational factors. The typical factor is stress. Chronic insomnia is most commonly caused by psychiatric disorders. Numerous medical disorders can cause insomnia. Many drugs have been implicated as causing insomnia alcohol, antihypertensives, antineoplastics, -blockers, caffeine, corticosteroids,...

Central Nervous System Stimulants

A huge number of physiologically active substances exhibit stimulatory action on the central nervous system (CNS) however, the number of drugs used for this purpose in medicine is extremely limited. Substances that increase vigilance and reduce the need for sleep are considered as CNS stimulants or psychostimulants. In other words, there are drugs capable of temporarily keeping one awake, elevating mood and maintaining adequate perception of reality, reducing outer irritability and the feeling...

Phenothiazine Derivatives

Phenothiazine derivatives are nonselective, competitive D1 and D2 antagonists that block dopamine activity on corresponding receptor sites. In addition, their action is expressed by blocking a-adrenoreceptors, serotonine, cholinergic, nicotinic, and muscarinic receptors. Phenothiazines exhibit a complex pharmacological range of action on the CNS and the peripheral nervous system. In addition, they act on the endocrine system. Every compound of this series differs to a certain degree from the...

Myotropic Hypotensive Drugs

The drugs of this class (hydralazine and sodium nitroprusside) lower arterial blood pressure primarily by direct spasmolytic action on smooth musculature of arterioles, which leads to a reduction of resistance of peripheral vessels by causing dilation. Diastolic pressure is usually lowered more than the systolic pressure. Hydralazine Hydralazine, 1-hydrazinonaphthalazine (22.6.4), is synthesized by the oxidative chlorination of phthalide with simultaneous hydrolysis of product, which results in...

Adrenergic Neuron Blockers

Adrenergic neuron blockers cause degradation of biogenic amines in neuron endings. These drugs can interfere with the synthesis, storage and release of norepinephrine, dopamine, and serotonin. Reserpine Reserpine is methyl ester acid (12.3.1). Reserpine is one of the alkaloids isolated from a perennial shrub of the Rauwolfia family 67-72 . It can also be synthesized 73-76 . Reserpine causes a breakdown of norepinephrine, dopamine, and serotonin in neuron endings. It weakens intracellular uptake...

Antihypertensive Drugs

Drugs that are used for treating hypertonic diseases as well as symptomatic hypertensions are called antihypertensive drugs. Hypertension is a syndrome characterized by elevated arterial blood pressure that depends on a number of factors. Some of the main factors that determine arterial blood pressure are parameters of heart rate, volume, viscosity, and electrolytic contents of circulating blood. Normal range of blood pressure varies depending on sex and age. Moreover, various medical schools...

Monoaminooxidase Inhibitors

Monoaminooxidase is a complex enzymatic system that is present in practically every organ that catalyzes deamination or inactivation of various natural, biogenic amines, in particular norepinephrine (noradrenaline), epinephrine (adrenaline), and serotonin. Inhibition of MAO increases the quantity of these biogenic amines in nerve endings. MAO inhibitors increase the intercellular concentration of endogenous amines by inhibiting their deamination, which seems to be the cause of their...

Insulin and Synthetic Hypoglycemic Agents

Drugs used for lowering the glucose level in the blood are called hypoglycemic agents. Likewise, substances that raise the level of glucose in the blood are called hyperglycemic agents. Changes in the level of glucose in the blood can be caused by various reasons, the primary cause being diabetes mellitus. Diabetes mellitus is a metabolic disease associated with a high level of blood sugar and as a rule, disturbance of carbohydrate, lipid, and protein metabolism. The most common biochemical...

Ganglioblocking Substances

Ganglioblockers are those compounds that selectively act on nerve transmission in the auto-nomic ganglia. (Theoretically, ganglioblockers can stop all autonomic activity in the organism). These drugs are classified as depolarizing and antidepolarizing ganglioblockers. Depolarizing ganglioblockers such as nicotine initially stimulate postganglionic receptors, and then they block subsequent activation of the receptor, thus preventing repolarization of the postsynaptic membrane. The...

Antimuscarinic Drugs

M-cholinoblockers are competitive antagonists of acetylcholine as well as other M-cholino-blockers in terms of postsynaptic M-cholinoreceptors. Parasympathetic cholinergic receptors are localized in smooth muscle of vessels, bronchi, gastrointestinal tract, urinary bladder, heart, ocular muscles, most of the exocrine glands, and in the CNS. M-cholinoblockers exhibit a wide spectrum of pharmacological effects and are used for a number of different indications. They can be used for causing...

Thiazide Diuretics

Most of the diuretics of the thiazide class are structurally related to antibacterial drugs of the sulfonamide class however, these compounds exhibit no antibacterial activity. Drugs of this group are derivatives of benzothiadiazine, and as a rule they are substituted at C7 of the benzol ring by a sulfonamide group and a chlorine atom, or by another electron-accepting group trifluoromethyl at C6. A hydrogenated thiadiazine ring of the benzothiadiazine system permits the introduction of various...

Immunopharmacological Drugs

The ability of the body to independently protect itself from certain diseases is called immunity. In a medical sense, immunity is a state of having sufficient biological defenses to avoid infection, disease, or other unwanted biological invasion. Immunity to certain diseases can be both inherent and acquired. Most types of immunity are either acquired during the course of life in response to infection by various microorganisms actively acquired immunity , or it can be attained by specific,...

Anticholinergic Drugs Central Cholinoblockers

The first drugs used in treating parkinsonism were the alkaloids, atropine and scopo-lamine, and over the course of many years they were the only drugs used for this purpose. However, in treating Parkinsonism today, these alkaloids are used extremely rarely and have been practically replaced by synthetic drugs that exhibit central anticholinergic properties central cholinoblockers . They suppress stimulatory cholinergic effects by suppressing cholinoreceptors. It is believed that they do not...

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Flucytosine is used with amphotericin for treating certain systemic fungal infections, in particular for treating subcutaneous chromobastomycosis. It is used intensively for treating systemic infections of the urinary tract that are caused by various strains of Candida. Synonyms of this drug are ancobon, ancotil, and others. Undecylenic acid Undecylenic acid, 10-undecylenic acid 35.4.7 , is synthesized by pyrolysis at 400 C and low pressure 50 mm an oxyderivative of oleic acid ricinoleic acid...

References

Pathol., 10, 226 1929 . 2. P.W. Clutterbuck, R. Lovell, H. Raistrick, Biochem. J., 26, 1907 1932 . 3. E. Chain, H.W. Florey, A.D. Gardner, N.G. Heatley, M.A. Jennings, J. Orr-Ewing, A.G. Sanders, Lancet, 2, 226 1940 . 4. E.P. Abraham, E. Chain, C.H. Fletcher, N.G. Heatley, M.A. Jennings, H.W. Florey, Lancet, 2, 177 1941 . 5. A.D. Lester, L. Somerson, U.S. Pat. 3.024.169 1962 . 6. J.C. Seehan, U.S. Pat. 3.159.617 1964 . 7. M.D. Bachi, S. Sasson, V.J. Sabar, J. Chem....