Calcium Channel Blockers

In addition to being used as antianginal and antiarrhythmic agents, calcium channel blockers are used to treat weak and moderate hypertension. These drugs prevent calcium ions from entering into the smooth muscle cells of peripheral vessels, and they cause relaxation of peripheral vessels, which leads to lowering of arterial blood pressure. In clinically used doses, calcium channel blockers relax smooth musculature of arteries and have little effect on veins. In doses that relax smooth...

Info

It is effective against Gram-positive cocci and staphylococci that produce penicillinase. It is used for the same indications as methicillin. Synonyms of this drug are nafcil, nalpen, unipen, and others. Another type of semisynthetic penicillin that should undoubtedly be considered is penicillin derivatives of heteroylcarboxylic acids (as a rule an isoxazol) in the third position of which is present a substituted or nonsubstituted phenyl radical (oxacillin, cloxacillin, dicloxacillin), which...

O

Buspirone is an extremely specific drug that could possibly represent a new chemical class of anxiolytics azaspirones. As an anxiolytic, its activity is equal to that of benzodi-azepines however, it is devoid of anticonvulsant and muscle relaxant properties, which are characteristic of benzodiazepines. It does not cause dependence or addiction. The mechanism of its action is not conclusively known. It does not act on the GABA receptors, which occurs in benzodiazepine use however, it has a high...

Ho

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...

Calcium Channel Activators

Minoxidil Minoxidil, (22.8.5), is synthesized from barbituric acid, the reaction of which with phosphorous oxy-chloride gives 2,4,6-trichloropyrimidine (22.8.1). Upon reaction with ammonium, this turns into 2,4-diamino-6-chloropyrimidine (22.8.2). Next, the resulting 2,4-diamino-6-chloropyrimidine (22.8.2) undergoes reaction with 2,4-dichlorophenol in the presence of potassium hydroxide, giving (22.8.3). Oxidation of this product with 3-chloroperbenzoic acid gives (22.8.4), the...

Diuretics

Hypertension therapy suggests wide use of diuretics, including thiazide diuretics, drugs related to them, such as metolazone (21.3.20) and indapamide (21.3.26), furosemide (21.4.11), loop diuretics, as well as potassium sparing diuretics spironolactone (21.5.8), triamterene (21.5.13), and amyloride (21.5.18). The molecular mechanism of diuretics acting as antihypertensive agents is not completely clear however, use of diuretics causes a significant increase in the amount of water and...

Antiparkinsonian Drugs

Parkinson's disease is a degenerative, slowly progressing illness of the CNS characterized by bradykinesia, shuffling gait, postural instability, tremor, and loss of automatic movement, which is associated with damaged basal ganglions. The etiology of this illness is not known. The most likely cause of the aforementioned motor problems could be a lack of dopamine, which has an inhibitory effect on the regulatory function of the spinal cord. On the other hand, cholinergic neurons act in...

References

Pat. 2.596.069 (1952). 2. J.E. Gasson, U.S. Pat. 2.830.994 (1958). 3. H. Pasedach, M. Seefelder, Ger. Pat. 1.116.667 (1956). 4. H. Meyer, G. Mally, Monatsh. Chem., 33, 393 (1912). 5. T.Urbanski, Z. Biernacki, D. Gurne, L. Malski, M. Mioduszeuska, B. Serafinova, J. Urbanski, D. Zelazko, Roca. Chem., 27, 161 (1953). 6. R.G. Wilkinson, R.G. Shepherd, U.S. Pat. 3.176.040 (1965). 7. L. Bernardi, O. Goffredo, Fr. Pat. 2.030.903 (1970). 8. Societa Farmaceutici Italie, Br. Pat....

Natural muscarinic alkaloids

Muscarine Muscarine, methylente-trahydrofuran chloride (13.1.14), was first isolated from the poisonous mushrooms Amanita muscaria. It can be synthesized in various ways from completely different substances 16-24 , particularly from 2,5-dimethyl-3-carboxymethylflurane, which undergoes a Curtius reaction, i.e. successive reactions with hydrazine and further with nitrous acid in isopropyl alcohol, which forms the urethane (13.1.9), the acidic hydrolysis of which gives 2,5-dimethyl-2H-furane-3...

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...

Angiotensinconverting Enzyme Inhibitors

Angiotensin-converting enzyme inhibitors have turned out to be very effective antihypertensive drugs that have begun to overtake -adrenoblockers, especially in monotherapy of hypertension. These drugs inhibit angiotensin-converting enzyme by blocking the hydrolysis of angiotensin I into active angiotensin II, which is an active, endogenic vasopressor substance. Angiotensin I is a prohormone that is formed as a result of the action of renin on a pep-tide substrate produced by the liver. Renin,...

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...

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...

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...

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...

Lcr

Histamine is synthesized in tissues by decarboxylation of amino acid L-histidine, a process catalyzed by the pyridoxalphosphate-dependent enzyme L-histidinedecarboxylase. Histamine can enter the organism with food it also can be generated by bacteria of the gastrointestinal tract. However, these sources do not create additional reserves of histamine since exogenous histamine is easily catabolized in the organism. Histamine is dispersed and stored in mast cells in the majority of organs, in...

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...

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...

Hh

Levodopa also is synthesized from piperonal, the aldehyde group of which is reduced by hydrogen over Raney nickel, forming a piperonyl alcohol, 3,4-methylendioxyphenyl-methanol (10.1.5). Upon reaction with hydrochloric acid, the product is transformed into 3,4-methylendioxyphenylmethylchoride (10.1.6). Reacting this compound with acetami-domalonic ester gives ester (10.1.7). Alkaline hydrolysis and partial decarboxylation of this product leads to the formation of the product (10.1.8) in which...

Loop Diuretics

Drug Ethacrynic Acid Synthesis

The most powerful diuretic effect is provided by loop diuretics, which severely inhibit reabsorption of sodium and chloride ions from renal tubules in cortical and cerebral regions and the ascending region of Henle's loop. In both oral and intravenous introduction, they cause a rapid rise in excretion of sodium and chloride ions from the kidneys and an increase in secreted urine volume. An increase in potassium, hydrogen, magnesium, and calcium ions is observed simultaneously with the increase...

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,...

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...

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,...

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,...

Antiviral Drugs

Antiviral drugs are a class of medication used specifically for treating viral infections. Like antibiotics, specific antivirals are used for specific viruses. Viruses cause more diseases than any other group of parasites. They can cause blindness, deafness, paralysis, mental retardation, various birth defects, and in at least a few plants and animals, cancer. Of all the most well-known viral diseases, the ones that should be stated are measles, mumps, smallpox, chicken pox, influenza,...

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...

Hypolipidemic Agents

Drugs that lower the concentration of lipoproteins in the plasma by inhibiting their production in the organism or by removing them from the plasma are called hypolipidemic or antisclerotic drugs. Atherosclerosis is a condition of the organism characterized by elevated levels of athero-genic lipoproteins in blood plasma, lipid deposits (including cholesterol) in the form of esters inside walls of the arterial system, and it is expressed by a gradual difficulty of blood circulation. The most...

Adrenergic Neuron Blockers

Guanethidine Synthesis

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...

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...

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...

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...

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...

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...

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...

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...

Temazepam Synthesis

Triazolam is the most frequently prescribed drug for insomnia. However, addiction to tri-azolam can develop very quickly, as can a number of other side effects such as early-morning insomnia, daytime anxiety, and others. Synonyms for this drug are normison, remstan, restoril, and others. Temazepam Temazepam, 4.2.7 , is synthesized from the intermediate product of oxazepam synthesis, zepin-2-on-4-oxide 5.1.17 , by methylation of the nitrogen of the amide group in the first position of the...

Dyz

Oxazepam is similar to chlordiazepoxide in terms of pharmacological properties however, it has a somewhat less harsh effect, is less toxic, and exhibits a less expressed myorelaxant effect. It is often tolerated better by patients than other tranquilizers. It is used in neurosis, conditions of anxiety, fear, stress, trouble falling asleep, and psychovegatative disorders. The most common synonyms are nozepam and tazepam. Lorazepam Lorazepam, 5.1.31 , is synthesized according to a scheme...

Cardiotonic Drugs

Drugs that increase the contractile power of the myocardium and thus enhance its capability and efficacy are called cardiotonic agents. This definition has traditionally referred to a group of drugs called cardiac glycosides strophanthin, digitoxin, digoxin however, new cardiotonic drugs nonglycoside cardiotonic agents that inhibit phosphodiesterases, amrinone, and milrinone that exhibit similar properties have recently been introduced into medical practice. Cardiac glycosides are drugs used in...