FIRM MEDICINAL FORMS Powders EXAMPLE. To write out 20,0 smallest powders of streptocide, to prescribe for drawing to a wound. Rp.: Streptocidi subtillissimi 20,0 D.S. For drawing on a wound EXAMPLE. To write out 30,0 magnesium oxide. To prescribe on m of a teaspoon 3 times a day in 2 hours after meal. Rp.: Magnesii oxydi 30,0 D.S. By teaspoon 3 times a day in 2 hours after meal EXAMPLE. To write out 10 powders of Codeini phosphas on 0,025 with soda. To prescribe on 1 powder 3 times a day. Rp.: Codeini phosphatis 0,025 Natrii bicarbonatis 0,3 M.f. pulvis D.t.d. N. 10 S. By 1 powder 3 times a day Cont. EXAMPLE. To write out 10 powders of camphor grated on 0,15 in a waxen paper. To prescribe on 1 powder 3 times a day. Rp.: Camphorae tritae 0,15 D.t.d. N.10 in charta cerata S. By 1 powder 3 times a day EXAMPLE to Write out 100,0 complex lacritic powder and to prescribe on 1 teaspoon 3 times a day. Rp.: Pulveris Liquiritiae compositi 100,0 D.S. By 1 teaspoon 3 times a day Sheaths EXAMPLE. To write out 10 powders of quinine of sulphate on 0,3 capsular gelatinous. To prescribe on 1 sheath 3 times a day. Rp.: Chinini sulfatis 0,3 D.t.d. N.10 in capsulis gelatinosis S. By 1 sheath 3 times a day Granules Rp.: Granulorum Natrii para-aminosalicylatis 100,0 D.S. By 1 teaspoon 3 times a day after meal Tablet EXAMPLE. To write out 10 tablets of Dimedrol on 0,03. To prescribe on 1 tablet 2 times a day. Rp.: Dimedroli 0,03 D.t.d. N. 10 in tabulettis S. By to 1 tablet 2 times a day EXAMPLE. To write out 10 tablets "Aeronum", to prescribe on 1 tablet 1-2 hours prior to flight. Rp.: Tabulettas “Aeronum” N. 10 D.S. By1 tablet 1-2 hours prior to flight Dragee EXAMPLE. To write out 20 dragees containing on 0,025 aminazine. To prescribe on 1 dragee 2 times a day. Rp.: Dragee Aminazini 0,025 D.t.d. N. 20 S. By 1 dragees 2 times a day Except all these firm medicinal forms exist also: To new medicinal forms concern - membranulae ophthalmicae Cont. EXAMPLE. To write out 30 ophthalmic Membranulas, containing Pilocarpinum a hydrochloride. To seat on 1 Membranula for edge of a lower eyelid of 1 times a day. Rp.: Membranulas ophthalmicas cum Pilocarpini hydrochlorido N. 30 D.S. To seat on 1 Membranula for lower eyelid edge daily If the drug is destroyed by stomach acid or is irritating to the mucous membrane of the stomach, it is prescribed in special dosage forms (capsules, pills) that are soluble only in the small intestine. Absorption of substances regulated as a special membrane transporter - P-glycoprotein. It promotes the excretion of substances into the lumen of the intestine and prevents their absorption. P-glycoprotein pump is also blood-brain barrier, kidney, liver, placenta and other tissues. Therefore, this transportation system affects many processes: absorption, distribution, elimination. Known inhibitors of P-glycoprotein - cyclosporin A, quinidine, verapamil, itraconazole, and many others. There is evidence that rifampin, an inducer of this transporter. Due to the fact that the substance developing a systemic effect only after getting into the bloodstream, where it enters the tissue is provided, the term "bioavailability". It reflects the amount of unchanged substance has reached the blood plasma, relative to the initial dose. In this case the bioavailability of enterally value determined lossy substance at its absorption from the digestive tract and first-pass hepatic barrier. To assess the bioavailability usually measure the area under the curve, which reflects the relationship between the concentration of the substance in the blood plasma and the time since the rate is directly proportional to the number of substances introduced into the systemic circulation. Also determine the maximum concentration of free (active) of the substance in the blood plasma and the time required to achieve it. Biodostupnost substance when administered intravenously as 100%. On bioavailability can be judged by the release of the drug in the urine, provided it is not subject to biotransformation. In some cases, the criterion may be the amount bioavailability pharmacological effect if applicable its precise quantitative measurement. With the introduction of the substance under the tongue sublingual (tablets, granules, drops) - suction starts pretty quickly. In this case, the drugs have general action, bypassing the first hepatic passage barrier and contact with enzymes and the environment of the gastrointestinal tract. Sublingual designate certain substances with high activity (single hormonal agents, nitroglycerin) where the dose is low. Sometimes drugs are administered by gavage to the duodenum (e.g., magnesium sulfate as a choleretic), which allows to quickly create a high concentration of gut connection. When administered into the rectum (per rectum) substantial part of the substance (about 50%) goes into the bloodstream, bypassing the liver. Moreover, in this way the introduction substance is not exposed to enzymes of the digestive tract. Absorption from the rectum occurs by simple diffusion. Rectally administered drugs into suppositories or enemas drug (volume 50 ml). If the substance is irritating effect, they are combined with mucus. Medicinal substances having the structure of proteins, fat and polysaccharides in the colon are not absorbed. Rectal use of substance and for local effects. For parenteral routes of administration include subcutaneous, intramuscular, intravenous, intraarterial, intrasternal, intraperitoneal, inhalation, subarachnoid, suboccipital and others. Parenteral routes of the most common is the introduction of substances under the skin, into the muscle and veins. Effect occurs especially quickly when administered intravenously, is somewhat slower - intramuscular and subcutaneous administration. In order to prolong the effect of pharmacotherapeutic drugs injected into a muscle in the form of poorly soluble (suspension) in oil or other grounds, delaying absorption of substances from the site of administration. Intramuscular and subcutaneous should not introduce substances which have a pronounced irritant effect, as this can cause inflammatory reactions and even necrosis infiltrates. Furthermore, in some reabsorption endogenous substances (amino acids, glucose, uric acid) participates actively transport. A number of drugs (tetracyclines, penicillins, phenytoin, colchicine, etc.) and especially the products of their transformation in a significant amount excreted in the bile into the intestine, where partially excreted in the feces and can be reabsorbed and subsequently re-released into the intestines, etc. . (The so-called enterohepatic circulation, or hepatic recirculation). Gaseous and many volatile matter (for example, the means for inhalation anesthesia) are displayed in the main light. Some drugs are excreted salivary glands (iodide), sweat (protivoleproznoe means ditofal) glands of the stomach (quinine, nicotine) and intestines (weak organic acids), lacrimal glands (rifampicin). It should also be borne in mind that in lactating mammary gland secretes many substances that receives nursing mother (hypnotics, sedatives, ethyl alcohol, nicotine, etc.). In this regard, care is required to appoint the mother of drugs, since the milk they can get into the child's body and have an adverse effect on him. Elimination (removal) of the substance of the body is provided by biotransformation and excretion. To quantify elimination process uses a series of parameters: elimination rate constant (K elim), «half life» (t1 / 2) and total clearance (CL T). The elimination rate constant (K eljm) reflects the rate of material removal from the body. To assess the clearance rate of substances from the body is used as the parameter "half-life" (elimination half-life) - t1 / 2, which reflects the time required for reducing the concentration of a substance in blood plasma by 50%. This parameter is used for the selection of doses of substances and intervals of administration to create steady-state concentration of the drug. It is known that the removal of substances of more than 90% is carried out for a time equal to four tl / 2, which is taken into account when dispensing. It should be borne in mind that the t1 / 2 is determined not only breeding material from the body, but also its biotransformation and deposition. Furthermore, to quantify the elimination rate substances used parameter clearance (CL) from the English. clearance - cleaning, reflecting the rate of plasma cleaning of the substance (expressed in volume per unit time, if necessary with the body weight or surface: ml / min ml / kg / min l/m2/ch etc.) . Allocate general (total), clearance (CL T), and kidney (CL R) and hepatic (CL H) clearance. The total clearance is associated with parameters such as volume of distribution (Vd), «half life» (t 1/2) and the elimination rate constant (K elim). Resorptive effect depends on the route of administration of drugs and their ability to cross biological barriers. At the local and resorptive effect drugs have either a direct or reflex effect. First implemented in place of direct contact of the substance with a cloth. When the reflex action of matter affect exteroanterocone or interoceptors and the effect is the change of state or the corresponding nerve centers, or executive. Thus, the use of yellow cards in the pathology of respiratory refreflex improves their trophic (mustard essential oil stimulates exteroceptors skin). The drug lobelia, injected intravenously, has a stimulating effect on the carotid chemoreceptors glomerulus and stimulating the reflex center of respiration, increases the volume and respiratory rate. The main objective of the pharmacodynamics - find out where and how the drugs are causing these or other effects. Thanks to the improvement of instructional techniques, these issues are not only at the system and organ, but also on the cellular, sub-cellular, molecular and submolecular levels. So, for neurotropic drugs applies the structure of the nervous system, synaptic formation of which have the most by a high sensitivity to these compounds. For substances that affect the metabolism is determined by the localization of enzymes in different tissues, cells and subcellular entities whose activity changes is particularly important. In all cases, we are talking about the biological substrates, "targets", which interact with the drug. As the "target" for the drug are receptors, ion channels, enzymes, transport systems and genes. Receptors called active groups of the macromolecules of substrates with which a substance. Receptors, providing the manifestation of substances called specific. There are the following 4 types of receptors. I. Receptors direct control over the function of ion channels. This type of receptor directly associated with ion channels, include n-cholinergic receptors, GABA receptors, glutamate receptors. II. Receptors associated with effector through «G-proteins - the secondary transmitter" or «G-protein-gated ion channels". These receptors are available for many hormones and neurotransmitters (m-cholinergic receptors, adrenergic receptors). III. Receptors directly control the effector function of the enzyme. They are directly related to tyrosine phosphorylation of proteins and adjusted. According to this principle arranged insulin receptors several growth factors. IV. Receptors controlling transcription of DNA. In contrast to membrane receptors type I-III is intracellular receptors (soluble cytosolic or nuclear proteins). With these receptors interact with steroid and thyroid hormones. Most fruitful study of receptor subtypes and associated effects. Among the first studies of this type include work on the synthesis of many in-blockers are widely used in various diseases of the cardiovascular system. Then came the histamine H2-blockers receptor - effective for the treatment of gastric ulcer and duodenal ulcer. Later it was synthesized in a variety of other drugs that act on different subtypes of alpha-adrenergic receptors, dopamine, opioid receptors, etc. These studies have played a major role in the creation of new groups of selective drugs, which are widely used in medical practice. Pharmacological interaction due to the fact that one substance or alters the pharmacokinetics (s) other components of the mixture pharmacodynamics. Pharmacokinetic interaction type can be associated with malabsorption, biotransformation, transport, deposition and removal of the substances. Pharmacodynamic type of interaction is the result of direct or indirect interaction of matter at the level of receptor cells, enzymes, organ or physiological systems. In this case, the main effect may vary quantitatively (amplified, attenuated) or qualitatively. In addition, the possibility of chemical and physico-chemical interaction of substances in their joint application. Pharmacokinetic type of interaction can occur at the stage of absorption of substances, which may vary for different reasons. Thus, in the digestive tract may be binding substances absorbent material (activated carbon, white clay) or anion-exchange resin (e.g. cholestyramine hypolipidemic agent), the formation of inactive chelate or chelates (for example, according to the principle tetracycline group of antibiotics interact with the ions of iron, calcium, magnesium). All of these forms of interaction prevents the absorption of drugs and thus reduce their pharmacological effects. For some substances absorption from the digestive tract is essential pH. So by changing the reaction of digestive juices, can significantly affect the rate and completeness of absorption of weakly acidic and weakly basic compounds General principles of treatment of acute poisoning by drugs Acute poisoning by chemicals, including drugs, are quite common. Poisoning may be accidental, intentional (suicide (from Lat. Suicidum - suicide (sui - myself, caedo - kill)) and associated features of the profession. Most common acute poisoning with ethyl alcohol, hypnotics, psychotropic drugs, opioid and non-opioid analgesics, organophosphate insecticides and other compounds. For the treatment of poisoning by chemicals created special poison control centers and offices. The main objective in the treatment of acute poisoning is to remove substances from the body, causing the toxicity. In severely ill patients it must be preceded by general therapeutic and resuscitative measures aimed at ensuring the functioning of vital systems - respiration and blood circulation. The principles of detoxification are as follows. First of all it is necessary to delay the absorption of the substance on the routes of administration. If the substance is partially or fully grown deep, should accelerate its excretion from the body, as well as take advantage of antidotes for its neutralization and elimination of adverse effects. a) delay absorption of the toxic substance in the blood If the substance to cause intoxication, is applied to the skin or mucous membranes, wash them thoroughly (preferably flowing water). After contact with toxic substances through the lungs should stop their inhalation (to remove the victim from the poisonous atmosphere or wear a gas mask on him). When subcutaneous absorption of toxic substances from its insertion site can slow injection of adrenaline solution around the site of administration, as well as by cooling in the area (the skin surface placed on an ice pack). If possible, the tourniquet is applied, obstructing blood flow and creating venous stasis in the administration of the substance. All of these measures reduce systemic toxic effects of the drug. b) removing the toxic substances from the body If a substance has grown deep and resorptive effect, major efforts should be directed to the early elimination from the body. For this purpose use diuresis, peritoneal dialysis, hemodialysis, hemosorption, blood substitution, etc. The method is forced diuresis combined aqueous active load using diuretics (furosemide, mannitol). In some cases the urine acidification or alkalization (depending on the properties of the material) contributes to more rapid removal of material (by reducing its reabsorption in the renal tubules). The method of forced diuresis can display only free agents not associated with proteins and lipids blood. Using this method should maintain electrolyte balance, which may be disrupted due to excretion of large amounts of ions. In acute cardiovascular insufficiency, severe renal dysfunction and the risk of developing cerebral edema or pulmonary forced diuresis is contraindicated. In addition to forced diuresis, using hemodialysis or peritoneal dialysis (dialysis (from the Greek. Dialysis - Branch) - separation of colloidal particles of the solute).