THE SOLUTIONS WHICH ARE DISCHARGE FOR INJECTIONS.

SOFT MEDICINAL FORMS

EXAMPLE: To write out Atropini sulfas (Td=0,001) in not parted and parted

kind all means hypodermic on 10 injections. Calculation: we write out on 10 injections on 1 ml on an injection Single dose=0,001 NOT PARTED MEAN 1. Rp.: Atropini sulfatis 0,01 (0,001 * 10) Aquae pro injectionibus 10 ml (1 ml * 10 ml) M.f. solutio Sterilis! D.S. By 1 ml subcutaneously

The solutions which are prescribing for an injection

2. Rp.: Sol. Atropini sulfatis ex 0,01 – 10 ml Sterilis! D.S. By 1 ml subcutaneously 3. Rp.: Sol. Atropini sulfatis 0,1% – 10 ml 100 -

x Sterilis!

10- 0,01 D.S. By 1 ml subcutaneously x=

100*0,01/10=0,1

Cont.

THE PARTED MEAN 1. Rp.: Atropini sulfatis 0,001 Aquae pro injectionibus 1 ml D.t.d. N. 10 in ampullis S. By 1 ml subcutaneously   2. Rp.: Sol. Atropini sulfatis ex 0,001 - 1 ml D.t.d. N. 10 in ampullis S. By 1 ml subcutaneously   3. Rp.: Sol. Atropini sulfatis 0,1% - 1 ml 1 - 0,001 D.t.d. N. 10 in ampullis 100 – x

S. By 1 ml subcutaneously x = 100*0,001/1=0,1

Cont.

EXAMPLES 1. To write out 10 % Calcii chloridum solution on 10 ml in

ampulas on 10 intravenous injections Rp.: Sol. Calcii chloridi 10% - 10 ml D.t.d. N. 10 in ampullis S. By 10 ml i.v. 2. To write out 200 ml of 0,9 % of an isoosmotic solution of

Sodium chloridum for i.v. introduction Rp.: Sol. Natrii chloridi 0,9% - 200 ml Sterilis! D.S. For intravenous introduction

Cont.

EXAMPLE Write out Solutio oleosa of camphor for hypodermic introduction (Td=0,2)

Rp.: Sol. Camphorae oleosae ex 0,2 – 1 ml D.t.d. N. 10 in ampullis S. By 1 ml hypodermic   Rp.: Sol. Camphorae oleosae 20% – 1 ml 1 -

0,2 D.t.d. N. 10 in ampullis 100- х S. By 1 ml hypodermic х=100*0,2/1=20

Cont.

EXAMPLES Write out 6 ampulas of Hexenalum on 1,0 and to prescribe on 1,0

for intravenous introduction, preliminarily having dissolved ampula contents in 10 ml of water for injections

Rp.: Hexenali 1,0 D.t.d. N.6 in ampullis S. Dissolve ampula contents in 10 ml of water for Injections and sluggishly inject into a vein before a

narcosis Rp.: Aquae pro injectionibus 10 ml D.t.d. N. 6 in ampullis S. For preparation of solution of Hexenalum

Cont.

2. Write out 10 vials Benzylpenicillini-sodium on 500000 ED and prescribe i.m. 4 times a day.

Rp.: Benzylpenicillini-natrii 500000 ED D.t.d. N. 10 S. Vial contents dissolve in 5 ml 0,25% sol. Novocainum and inject i.m. 4 times a day Rp.: Sol. Novocaini 0,25% - 5 ml D.t.d. N. 10 in ampullis S. For dissolution benzylpenicillini

Cont.

EXAMPLE Write out 100 ml Biiochinolum and prescribe on 3 ml i.m. 1 time in 3 days. Shake before useing Rp.: Biiochinoli 100 ml D.S. By 3 ml i.m. 1 time in 3 days. Shake before using EXAMPLE 1. Write out 10 ampulas of Cordiaminum on 1 ml and prescribe on 1 ml subcutaneously

once a day Rp.: Cordiamini 1 ml D.t.d. N. 10 in ampullis S. By 1 ml subcutaneously once a day 2. Write out 10 ampulas digalen-neo by 1 ml and prescribe by 1 ml subcutaneously once a day Rp.: Digalen-neo 1ml D.t.d. N. 10 in ampullis S. By 1 ml subcutaneously once a day 3. Write out 10 ampulas containing 1 ml (5 ED) Pituitrinum. Prescribe by 1 ml hypodermic. Rp.: Pituitrini 1 ml D.t.d. N. 10 in ampullis S. By 1 ml hypodermic

Cont.

EXAMPLE to Write out 20,0 ointments on Vaselinum with the maintenance of 10 % of zinc oxide

Calculation: 100 - 10 20 - х х=20*10/100=2 Rp.: Zinci oxydi 2,0 Vaselini ad 20,0 M.f. unguentum D.S. For greasing of the damaged field of a skin EXAMPLE: Rp.: Unguenti Zinci oxydi 10% - 20,0 D.S. For greasing of the damaged field of a skin EXAMPLE Write out 10,0 officinal Unguentums Zinci. Rp.: Unguenti Zinci 10,0 D.S. For greasing of the damaged field of a skin

Ointment

EXAMPLE Write out 50,0 Pastas, keeping 5 % of Anaesthesinum and 25 % of Zinci oxydum.

Calculation: 100 - 5 50 - х х= 50*5/100=2.5 Anaesthesinum 100 – 25 50 - х х=50*25/100=12,5 Zinci oxydum Rp.: Anаesthesini 2,5 Zinci oxydi 12,5 Vaselini ad 50,0 M.f. pasta D.S. For greasing of the damaged field of a skin

Pasta

EXAMPLE to Write out 75 ml of Linimentum with the maintenance of turpentine of 5 % and 15 % Methylii salicylatis

Calculation: 100 – 5 75 - х х=75*5/100=3,75 turpentine   100 – 15 75 - x x=75*15/100=11,25 Methylii salicylatis Rp.: Olei Terebinthinae 3,75 Methylii salicylatis 11,25 Olei Gossypii ad 75 ml M.f. linimentum D.S. For grinding EXAMPLE: Write out 25 ml officinal 5 % of Linimentum Synthomycini Rp.: Linimenti Synthomycini 5% - 25 ml D.S. Put on a wound

Linimentum

EXAMPLE to Write out 10 rectal suppositories, containing on 0,3 Anaesthesinums. To prescribe on 1 suppository in the morning and in the evening.

Rp.: Anaesthezini 0,3 Olei Cacao 3,0 M.f. suppositorium rectale D.t.d.N. 10 in charta cerata S. By 1 suppositories 2 times a day in a rectum   Rp.: Suppositorium cum Anaesthezino 0,3 D.t.d. N. 10 in charta cerata S. . By 1 suppositories in the morning and in the

evening

Suppositories

This is the most convenient and simple way of introduction. Sterile preparation in this case not needed. Absorption (absorption) of a number of substances (for example, acetylsalicylic acid, barbiturates, and other weak electrolytes that are acidic in nature) is part of the stomach (in the acidic environment of the stomach, these compounds are found mainly in the non-ionized (lipophilic) form and are absorbed by diffusion). However, the vast majority of drug is absorbed mainly in the small intestine. This favorable large suction surface of the intestinal mucosa (approx. 200 m2) and its intense perfusion. Known basic mechanisms of absorption:

1. Passive diffusion across the cell membrane. Determined by the gradient of concentration of substances. In this way easily absorbed lipophilic (mostly nonpolar) substance. The more lipophilic substances, they are more easily penetrate through the cell membrane (so-called isolated facilitated diffusion. It involves transport system functioning without energy loss). 2. Filtration through membrane pores. The pore diameter of the membrane of the intestinal epithelium is small (about 0.4 nm). Therefore, water diffuses therethrough, some ions and small hydrophilic molecules (e.g., urea). 3. Active transport (involved in this process of cell membrane transport systems) is characterized by selectivity for certain compounds, the possibility of competition between two substances in a single transport mechanism saturability (at high concentrations), the possibility of transport against a concentration gradient and energy expenditure (metabolic poisons inhibit active transport) . Active transport provides hydrophilic absorption of polar molecules, some inorganic ions, sugars, amino acids, pyrimidines.

4. When pinocytosis cell membrane invagination occurs with the consequent formation of the bubble (vacuoles). Last full of liquid with entrained large molecules of substances. Bubble migrates through the cytoplasm to the opposite side of the cell, wherein the contents by exocytosis bubble is expelled. These mechanisms of passage of substances through the membrane are universal in nature and are not only important for the absorption of substances, but also for their distribution in the body and excretion. The main mechanism of drug absorption in the small intestine is passive diffusion. Minor role played by active transport. Filtration through a cellular membrane pores virtually irrelevant. Absorption of certain proteins and complex cyanocobalamin (vitamin B12) to biermerin is apparently by pinocytosis. Absorption from the small intestine is relatively slow. It depends on the functional state of the intestinal mucosa and its motility and pH, the quantity and quality characteristics of the intestinal contents. It is important to bear in mind that the substance from the small intestine to the liver (where part of inactivated or excreted in bile) and only then - in general circulation. Note that some substances inside ineffective when assigning as degraded by the enzymes of the gastrointestinal tract (e.g., insulin), as well as the particular reaction medium, especially in acidic environment of the stomach (e.g., penicillin).

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.

Intravenously administered drugs are usually slow. Possible single, fractional, and a drip infusion. Should not be administered intravenously insoluble compounds, oil solutions (possibility of embolism), funds with a strong irritant (could lead to the development of thrombosis, thrombophlebitis), drugs that cause blood clotting or hemolysis. Negative aspects of these three routes of administration are their relative complexity and morbidity, the need for sterile preparations and participation of medical personnel. Intra-arterial injection can create in the area of the artery that supply blood to high concentrations of the substance. In this way, sometimes introducing an antineoplastic. In order to reduce their overall toxicity blood flow may be artificially difficult (by compression of veins). Also administered intra-radiopaque agents that can accurately determine the location of the tumor, blood clot, constriction of blood vessels, the aneurysm. Intrasternal injection path (in the sternum) is usually used in technical impossibility intravenous (children, elderly people). Intraperitoneal formulations administered infrequently (for example, antibiotics during celiac operations). Sometimes the medicines prescribed intrapleural (the pleural cavity). For gaseous and volatile compounds is a major inhalation route of administration. In the same way, and some are administered aerosols. Light - a vast absorption band (90-100 m2), receives abundant blood supply, so the absorption of substances from inhalation is rapid. The severity of the effect is easily controlled by changing the concentration of substances in the breathing air.