Pharmacology Concepts 2

Compiled by Venina Navuta 22/8/11

Terminology
Drug: substance or chemical that

alters physiological or biochemical pattern. Used in diagnosis, prevention or treatment. Drug action: interaction of drug with specific sites cells, receptors or at sub cellular level. (Usually Invisible) Drug effect: consequences of drug actions leads to notable change like

 Agonist: has affinity to specific

receptors where it exhibits its action (intrinsic activity) Antagonist: binds to the receptors of agonist and lacks activity Partial agonist: has some less affinity and less intrinsic activity. Has same actions as agonist but of less degree at the same time blocks the receptor for agonist to bind.

 Efficacy the ability to produce

aresponse Potency the dose range over which a response is produced Tachyplaxis a decrease in the response to a drug due to previous exposure to that drug Therapeutic index the ratio between the toxic dose and the therapeutic dose of a drug used as a measure of the relative safety of the drug for a particular

Dose-Response Relationship
Relationship between the size of an

administered dose and the intensity of the response produced The dose-response relationships for most drugs are graded i.e. response gets more intense with increasing dosage Because they are graded, therapeutic effects can be adjusted to fit the needs of each patient

Types of drug responses

For drug to act should reach a critical

concentration at its site of action Above critical concentration. Drug exhibits response related to dose up to certain range till its maximum therapeutic response is reached Once maximum drug response is reached rise in dose has no enhancement in response but leads to increase in toxic effects.

3 Phases of Dose-response relationship

Phase 1 occurs at low doses, too low to

elicit a measurable response Phase 2 - an increase in dose elicits a corresponding increase in the response. This phase is where dose-response relationship is graded Phase 3 a point where an increase in dose is unable to elicit a further increase in response, the curve flattens

Maximal Efficacy & Relative Potency Maximal efficacy the largest effect that a drug can produce Indicated by the height of the doseresponse curve drug with high maximal efficacy is not always more desirable than a drug with lower efficacy

Relative Potency
Amount of drug that we must give in

order to elicit an effect Potent drug is one that produces its effects at low doses Potency and efficacy are 2 independent qualities.

Drug-Receptor Interactions
Drugs are chemicals and the only way

to produce effects is by interacting with other chemicals Receptor a molecule which interacts with a ligand (drug) to mediate a pharmacologic effect. Receptors can be proteins, carbohydrates, nucleic acids or lipids.

 Receptors through which drugs act

are normal points of control of physiologic processes The two main functions of receptors are: ligand (drug) binding, and, activation of effector mechanism

 Under physiologic conditions, receptor

function is regulated by molecules supplied by the body All that drugs can do at receptors is mimic or block the action of bodys own regulatory molecules

 Drugs cannot give cells new function

but can only alter the rate of preexisting processes Drugs produce their therapeutic effects by helping the body use its pre-existing capacities to the pts best advantage. Medications simply help body to help itself

 In theory, it should be possible to

synthesize drugs that can alter rate of any biologic processes for which receptors exist Ligand binding is determined by affinity and specificity Affinity describes how strongly the drug and receptor interact. Specificity refers to selectivity a receptor has for a drug.

Agonists & Antagonists

Agonists bind to receptor sites & activate receptor mechanisms (elicit biological responses). Antagonists bind to receptors but do not activate effector mechanisms (do not produce biological effects)

Effectors
Transduce drug-receptor interactions into cellular effects. 1. Intracellular receptors 2. Transmembrane receptors 3. Ligand-gated ion channels 4. Receptors coupled to 2nd messenger systems

Individual Variations in Drug Responses

In order to maximize beneficial drug

responses & minimize harm, we must adjust therapy to account for sources of individual variation small pts need smaller doses than large pts Dosage adjustments made to account for size are often based on body surface area, rather than simply on body weight

 Infants & the elderly are more

sensitive to drugs Therapeutic & adverse effects differ between males & females Kidney disease can decrease drug excretion Liver disease can reduce drug metabolism

 When pts become tolerant to a drug,

dosage must be increased to maintain beneficial effects Placebo effect is `the component of a drug response that can be attributed to psychologic factors

 Genetic factors especially genetically

determined rates of drug metabolismcan be a source of individual variation Poor patient compliance is a major source of individual variation.

Classification of Drugs
Adrenergic
Dopaminergic Cholinergic Drugs Anticholinergic Drugs Calcium Channel Blockers

Ace Inhibitors

 Angiotensin II Inhibitors Opioids analgesics

Proton Pump Inhibitors

Corticosteroids Steroids