Pharmacology :- Pharmacology is the study of interaction of drugs with living organism. It includes history , source, physicochemical properties, dosage forms, methods of administration,absorption,distribution, mechanism of action, biotransformation, extretion,clinical uses and adverse effects of drugs. What Are Drugs? Drugs are synthetic chemical substances that can affect our body and its processes, our behavior and feelings Sources of drugs:- Drugs may be obtained from Plants ,Animals,Mineral / Earth sourcess ,Synthetic / Semi- synthetic sources , Microbiological sources and by Genetic engineering. TYPES OF DRUGS 6 TYPES OF DRUGS PRESCRIPTION DRUGS- those that can only be obtained through a written prescription. OVER-THE-COUNTER DRUGS- can be purchased without a prescription. RECREATIONAL DRUGS- drugs used to help a person relax or socialize. ex. Alcohol, Tea, Coffee, Tobacco, Chocolate HERBAL PREPARATIONS- Products of botanical(plant) origin that are believed to have medicinal purposes. ILLICIT DRUGS- these are the most notorious type of drugs. Generally, recognized as harmful. All are PSYCHOACTIVE (have the potential to alter mood or behavior) COMMERCIAL DRUGS- Most commonly recognized drugs. There are more than 1,000 of these. ex. Perfumes, cosmetics, household cleaners, paints, glues, inks, dyes, gardening chemicals, pesticides, and industrial by-products. PHARMACO KEINETICS Definition : The term pharmacokinetics is derived from two Greek words: pharnakon (drug or poison) and kinesis (motion). As this derivation implies, pharmacokinetics is the study of drug movement throughout the body Four Basic Pharmacokinetic processes: 1) Absorption 2) Distribution 3) Metabolism 4) Excretion These four processes determine the Concentration of drug at its site of action -Bioavailability
2 ABSORPTION :- Absorption is the movement of a drug from its site of administration into the blood. The rate of absorption determines how soon effects will begin and the amount of absorption helps determine how intense effects will be. Factors Affecting Drug Absorption :- The important factors that affect the absorption are i Rate of Dissolution ii Surface Area iii Blood Flow iv Lipid Solubility v P H Partitioning The routes of administration that are used most commonly fall into two major groups: Enteral (via the gastrointestinal tract) Parenteral. The literal definition of parenteral is outside the GI tract. Routes of administration Adventage Disadvantage Enteral 1) Oral (Through the mouth)
2) Rectal (as suppository)
3) Sublingual (underneath the tongue) Ease of use, Outpatient care Lower cost
Relative ease of use, Outpatient care,low cost,No effect of food, No effect of PH
Relatively ease of use, Outpatient care, Rapid onset of action, bypass stomach and intestine, No first pass effect Most complicated path, most variable response,effect of food in the stomache,Gastric PH,First pass effect
Complicated path, variable response, first pass effect (less)
More expensive,Taste, Limited available formulations Other roots
1) Transdermal (across the skin or skin patch)
2) Topical (Delivering a drug directely to its site of action)) Eg- Eye dropes) 3) Inhalation (breathing medication)
4) Intra nasal ( through nose)
Applied to the skin for systemic absorption for effect,Bypass First pass effect, Improved compliance
Rapid delivery over large surface area of respiratory tract Lower metabolism in lung tissue
3 First Pass Effect :- The orally administered drugs usually absorbed in G I Tract and the absorbed drug will enter in to the liver through Portal Vein . In the liver the drug gets metabolized before it reaches to the Portal circulation. This process is called First Pass effect DISTRIBUTION Distribution is defined as the movement of drugs throughout the body. Drug distribution is determined by three major factors: Blood flow to tissues ,The ability of a drug to exit the vascular system,The ability of a drug to enter cells. Blood Flow to Tissues:-In the first phase of distribution, drugs are carried by the blood to the tissues and organs of the body. The rate at which drugs are delivered to a particular tissue is determined by blood flow to the tissue. Exiting the Vascular System :- After a drug has been delivered to an organ or tissue via the blood, the next step is to exit the vasculature. Since most drugs do not produce their effects within the blood, the ability to leave the vascular system is an important determinant of drug actions. Exiting the vascular system is also necessary for drugs to undergo metabolism and excretion. Drugs in the vascular system leave the blood at capillary beds. Entering Cells :- Some drugs must enter cells to reach their sites of action, Practically all drugs must enter cells to undergo metabolism and excretion. The factors that determine the ability of a drug to cross cell membranes are the same factors that determine the passage of drugs across all other membranes, namely, lipid solubility, the presence of a transport system, or both. METABOLISM Known as biotransformation, is defined as the enzymatic alteration of drug structure. Most drug metabolism takes place in the liver Therapeutic Consequences of Drug Metabolism Drug metabolism has six possible consequences of therapeutic significance: Accelerated renal excretion of drugs , Drug inactivation , Increased therapeutic action Activation of "prodrugs" Increased toxicity and Decreased toxicity Accelerated Renal Drug Excretion The most important consequence of drug metabolism is promotion of renal drug excretion. The kidney, which is the major organ of drug excretion, is unable to excrete drugs that are highly lipid soluble.
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Drug Inactivation Drug metabolism can convert pharmacologically active compounds to inactive forms. This process is illustrated by the conversion of procaine (a local anesthetic) into paraaminobenzoic acid (PABA) an inactive metabolite Increased Therapeutic Action Metabolism can increase the effectiveness of some drugs. This concept is illustrated by the conversion of codeine into morphine. The analgesic activity of morphine is so much greater than that of codeine that formation of morphine may account for virtually all the pain relief that occurs following codeine administration Activation of Prodrugs Increased or Decreased Toxicity By converting drugs into inactive forms, metabolism can decrease toxicity. Conversely, metabolism can increase the potential for harm by converting relatively safe compounds into forms that are toxic. Increased toxicity is illustrated by the conversion of acetaminophen Tylenol, into a hepatotoxic metabolite. It is this product of metabolism, and not acetaminophen itself, that causes injury when acetaminophen is taken in overdose If the capacity of the liver to metabolize a drug is extremely high, that drug can be completely inactivated on its first pass through the liver. As a result, no therapeutic effects can occur. Nutritional Status. Hepatic drug-metabolizing enzymes require a number of cofactors to function. In the malnourished patient, these cofactors may be deficient, causing drug metabolism to be compromised. Competition Between Drugs
EXCRETION Drug excretion is defined as the removal of drugs from the body. Drugs and their metabolites can exit the body in urine, bile, Sweat, saliva, breast milk, and expired air. The most important organ for drug excretion is the kidney. Renal Drug Excretion The kidneys account for the majority of drug excretion. When the kidneys are healthy, they serve to limit the duration of action of many drugs. Renal failure - both the duration and intensity of drug responses may increase