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Pharmacology – Part I (4 CFU, 48 hours) – I semester General concepts Pharmacodynamics Pharmacokinetics Toxicology notions - Adverse drug reactions and pharmacogenetics
Cardiovascular Pharmacotherapy Antihypertensive drugs, anti-angina, antiarrhythmics, cardiotonics. Diuretics. Anticoagulants. Anti-hyperlipidemia drugs. Insulin and hypoglycemic agents
Pharmacotherapy (6 CFU, 72 hours) – II semester
Chemotherapy Parasitic diseases, microbial diseases, neoplastic diseases, immunotherapy Hematopoietics , antitumor hormonal therapy
Neuropharmacology General anesthetics, local anesthetics, hypnotics and sedatives (BZD, ethanol, ecc), anticonvulsants, analgesics (FANS, opioids, adjuvants), anti-neurodegeneratives (Parkinson, Alzheimer, dementia, others), psychiatric disorders. Drugs acting on peripheral nervous system: cholinergic agonists, anticholinesterase agents, antimuscarinic agents, catecholamines and sympathomimetic drugs, adrenergic receptor drugs. Drug addiction
Pharmacotherapy (others) Anti-inflammation (histamine antagonists, eicosanoids, PAF, treatment of asthma, FANS) , immunosuppression Gastrointestinal function (anti-ulcer, etc…), antiemetic agents, uterine motility Hormones and antagonists (Thyroid, estrogens, androgens, progestins, ADH). Bone and calcification. Vitamins
PHARMACOLOGY – V YEAR Prof. Jean François DESAPHY Prof. Monica MONTAGNANI
The science that deals with the origin, nature, chemistry, effects, and uses of DRUGS
PHARMACOLOGY
PHARMACOKINETICS What the body does to the drug
PHARMACODYNAMICS What the drug does to the body
PHARMACOTHERAPEUTICS Studies the use of drugs
PHARMACOGNOSY Identifies crude materials as drugs
TOXICOLOGY Studies the poisoning effects of drugs
PHARMACOLOGY
It includes pharmacognosy, pharmacokinetics, pharmacodynamics, pharmacotherapeutics, and toxicology.
WHO definition: “Natural or synthetic substance which is used or intended to be used to modify or explore physiological systems or pathological states for the benefit of the
recipient”.
Any substance that, when taken into a living body, affects its functioning or structure, and is used in the diagnosis, mitigation, treatment, or prevention of a disease or relief
of discomfort.
Remedy
Toxic or poison
DRUG
φάρμακον
DRUG: REMEDY, TOXIC OR POISON?
REMEDY: A drug can be used for the CURE when, administered in a patient with a pathological condition, is able to restore health, reduce pain or prevent complications.
REMEDY: A drug can be used for the PREVENTION: when, administered in a healthy subject, is able to hinder the onset or mitigate the progression of a pathological condition.
TOXIC: any substance when taken at inappropriately high doses or concentrations.
POISON: a chemical substance with no beneficial effects, even when dose or concentration is very low (snake poison, poison mushrooms, heavy metals).
Paracelsus (1493-1541)
"All things are poison and nothing is without
poison, only the dose permits something not to
be poisonous."
“The dose makes the poison”
DRUG NAME
Every marketed drug has at least three names - A CHEMICAL (SYSTEMATIC) NAME: the chemical name describes the atomic or molecular structure of the drug. This name is usually too complex for general use.
- A GENERIC (NON PROPRIETARY) NAME: the generic name identifies the drug internationally. Generic drugs are required to have the same active ingredient, strength, dosage form, and route of administration as the brand name product. Generic drugs do not need to contain the same inactive ingredients as the brand name product.
- A PROPRIETARY (BRAND) NAME: the brand name is selected by manufacturer or distributor of the drug. It is usually shorter and easier to remember than the generic name. The brand name of a drug implies that the drug is protected by a patent (can be produced and sold only by the company holding the patent)
Example:
N-(4-hydroxyphenyl)ethanamide N-(4-hydroxyphenyl)acetamide
CHEMICAL (SYSTEMATIC) IUPAC NAME
NON-PROPRIETARY (GENERIC) NAME
Approved name: BAN Paracetamol USAN Acetaminophen
Official name: BAN Paracetamol USAN Acetaminophen
PROPRIETARY (BRAND) NAME
Tachipirina® Efferalgan®
Zerinol® Perfalgan®
Tylenol®
WHAT IS A MEDICAL DRUG?
ACTIVE INGREDIENT (PRINCIPLE): a constituent of a drug, usually an alkaloid or glycoside, that is largely responsible for conferring its characteristic therapeutic properties EXCIPIENT (BULKING AGENT): an inactive substance that serves as the vehicle or medium for a drug or other active substance. Excipients are things like colouring agents, preservatives, and fillers.
ACTIVE INGREDIENT EXCIPIENT
WHAT IS A PRODRUG?
A PRODRUG is usually a pharmacologically inactive derivate of a parent drug that must undergo chemical conversion by metabolic processes before becoming an active
pharmacological agent. PRODRUG/DRUG TRANSFORMATION MAY BE ENZYMATIC AND NON-ENZYMATIC
A prodrug might be used instead of the active drug to
- mask taste or odor; minimize pain
- improve how a medical drug is absorbed, distributed, metabolized, and excreted (ADME).
- improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract.
- improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects.
WHAT IS A PLACEBO?
A PLACEBO is a simulated or otherwise medically ineffectual treatment for a disease or other medical condition, intended to deceive the recipient.
Persons given such an ineffectual treatment will often have a perceived or actual improvement in their condition, a phenomenon commonly called the placebo effect or placebo response. Several different elements contribute to the effect, and the methods of placebo administration may be as important as the administration itself.
Nocebo is an inert substance or treatment that appears to cause an adverse effect on a patient or participant although it has no known biological effect.
CLASSIFICATION OF DRUGs
Drugs can be classified according to multiple parameters.
- CHEMICAL NATURE
- SOURCE
- TARGET ORGAN/SITE OF ACTION
- MODE OF ACTION
- THERAPEUTIC USE
- PHYSIOLOGICAL SYSTEM / PHYSICAL EFFECTS
Biological drugs: Drugs made in/from
living organisms
A biosimilar drug (biologic) is NOT exactly a bioequivalent (generic)
USE of MEDICAL DRUGS
ETIOLOGY THERAPY: any medical treatment that aims at preventing or curing the causes of the disease
SYMPTOMATIC THERAPY: any medical treatment that aims at reducing the signs and
symptoms of the disease for the comfort and well-being of the patient, but also for reducing organic consequences and sequelae of the disease.
REPLACEMENT THERAPY: any medical treatment that aims at substituting and reintegrating the missing factor underlying the disease
ETIOLOGY DRUG SYMPTOMATIC DRUG REPLACEMENT DRUG
USE of MEDICAL DRUGS cont’d
OFF-LABEL USE: the use of pharmaceutical drugs for an unapproved indication or in an unapproved age group, dosage, or route of administration. A patient’s informed consent is requested and the MD is responsible (and can be prosecuted) for any side effect
COMPASSIONED USE: also called expanded access, provides access to unapproved investigational drugs, biologics and medical devices for patients with life-threatening conditions. According to The European Medicines Agency (EMA), compassionate use is defined as “the use of an unauthorized medicine outside a clinical trial in individual patients under strictly controlled conditions”.
It requires approval from the Ethic Committee and the MD accepts all the legal responsibilities
HOST
DISEASE DRUG
THERAPHY
DRUG RESISTANCE
INTERACTION DRUG-DISEASE
INTERACTION HOST- DISEASE
INTERACTION DRUG - HOST
INTERACTION DRUG BODY DISEASE
PHARMACODYNAMICS
Receptors - intracellular receptors - membrane receptors
- Channel receptors - G protein-coupled receptors - Tyrosine-kinase receptors
Drug/receptor interactions - agonists and antagonists - potency and efficacy (effectiveness) - therapeutic index
Drug effects - therapeutic effects - side effects - toxic effects
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