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Introduction to Pharmacology

Lecture 1 Pharmacology for Nursing


Utilize nomenclature Major Drug Classifications Identify Resources for Information Legal/Ethical Considerations Calculate Dosages

Pharmacology
Deals with the mechanism of action, uses adverse effects and fate of drugs in animals and in humans. Pharmakon refers to the study of what biologically active chemical compounds do in the body, and how the body reacts to them.
What is the difference between

Pharmacokinetics

Pharmacognosy

Science of
Pharmacology

Pharmacodynamics

Toxicology

Pharmacotherapeutics

Different Branches of Pharmacology


Pharmacolodynamic Pharmacokinetic Pharmacotherapetics Clinical Pharmacology Pharmacogenetics Pharmacovigilance Pharmacoeconomics Toxicology

Drugs and Drug Products


Drugs is a chemical xenobiotics substances that exerts a selective biological activity, it is a substance that is listed in the national pharmacopeia of a country (USP,BNF,PNDF) Drug Product is the commercial preparation of a drug having the active ingredients and the inactive ingredients

Terminology for Patients

Drug (medication)
pharmacological agent produces biological effect

Prescription Drug
safe under supervision prescribed by licensed practitioner

Terminology (cont)

Non-Prescription (Over-the-Counter or OTC)


safe if instructions followed no prescription necessary

Terminology (cont)

Recreational Drug
use for pleasant psychological/physical effects no therapeutic intent

Drug Nomenclature (Names)

Chemical Name
atomic/molecular structure

Generic Name (OFFICIAL)


derived from chemical name listed in US Pharmacopedia & Formulary

Trade Name (Brand)


selected by Manufacturer copyrighted

Drug Nomenclature (Names)


Chemical Name
7-chloro-1,3-dihydro-1methyl-5 phenyl 2H-1, 4-benzodiazepin 2-one Ethyl 1-methyl 4-pheylisonipecotate hydrochloride

Generic Name Trade Name


diazepam meperidine Valium Demerol

acetylsalicyclic aspirin

Ecotrin

Drug Classifications

Pharmacologic Classification
Similar Characteristics Similar Chemical Make up examples: Penicillins, Beta Blockers

Therapeutic Classification
Used for similar effect May not have similar chemical make up Examples: Antihypertensives, Antibiotics

Drug Classification
Origin of Source Chemical Structure Physiologic Use Therapeutic Use Anti Pathogens Function Modifiers Restoratives

Therapeutic Effects
Category O Category I Category II Category III Category IV Category V Disease Prevention Disease Etiology Specific Disease Processes
Specific Disease Manifestations
Non Specific Disease Manifestation

Non Therapeutic Drug Use

Pregnancy Category
A Controlled studies show no risk-Adequate, well-controlled studies in pregnant women have failed to demonstrate a risk to the fetus in any trimester of pregnancy. B No evidence of risk in humans-Adequate, well controlled studies in pregnant women have not shown increased risk of fetal abnormalities despite adverse findings in animals, or In the absence of adequate human studies, animal studies show no fetal risk. The chance of fetal harm is remote, but remains a possibility. C Risk can not be ruled out- Adequate, well-controlled human studies are lacking, and animal studies have shown a risk to the fetus or are lacking as well. There is a chance of fetal harm if the drug is administered during pregnancy; but the potential benefits may outweigh the potential risk. D Positive evidence of Risk-Studies in humans, or investigational or post marketing data, have demonstrated fetal risk. Nevertheless, potential benefits from the use of the drug may outweigh the potential risk. For example, the drug may be acceptable if needed in a life threatening situation or serious disease for which safer drugs cannot be used or are ineffective. X Contraindicated in Pregnancy- Studies in animals or humans, or investigational or post-marketing reports, have demonstrated positive evidence of fetal abnormalities or risk which clearly outweighs any possible benefit to the patient.

Philippine National Drug Formulary and Relevant Laws


It is the governments response to the problem of inadequate provision of good quality essential drugs to the people. The Five Pillars of PNDFP:
The assurance of the safety, efficacy and usefulness of pharmaceutical products through quality control. The promotion of the rational use of drugs by both health professionals and the general public. The development of self reliance in the local pharmaceutical industry. Tailored of targeted procurement of drugs by the government People empowerment

Philippine National Drug Formulary and Relevant Laws


Republic Act 6675 Generics Act of 1988
Aims to promote, require and ensure the production of an adequate supply, distribution, use and acceptance of drugs and medicines identified by their generic name. generics name are those scientifically and internationally recognized by their active ingredients or official name as determined by the DFAD of the DOH.

Republic ACT 9502 Cheaper Medicine Act Republic Act 6425 Dangerous Drug Act
Narcotics are drugs which produce insensibility, stupor, melancholy, delusion or dullness of mind and which may be habit forming. Prohibited Drugs Opium and its active components and derivatives such as heroin and morphine
coca leaf and its derivatives Alpha and beta cocaine Hallucinogens drugs like mescaline, lysergic acid diethylamide Indian hemp Self inducing sedatives Amphetamines Hypnotic drugs

Regulated drugs

Antibiotics
Aminoglycosides Cephalosphorins Flouroquinolones Macrolides Lincosamides MonoBactam Penicillins Penicillinase Resistant Antibiotic Sulfonamides Tetracyclines Anti Mycobacterial Antibiotics

Aminoglycosides
The aminoglycosides are the mainstay in the treatment of serious gramnegative systemic infections. A disadvantage of the aminoglycosides is their association with nephrotoxicity and ototoxicity, both of which are associated with elevated trough levels and sustained elevated peak levels. Aminoglycosides have bactericidal activity against most gram-negative bacteria including Acinetobacter, Citrobacter, Enterobacter, E. Coli, Klebsiella, Proteus, Providencia, Pseudomanas, Salmonella, Serratia and Shigella.

Amikacin Gentamicin Kanamycin Neomycin Streptomycin

Aminoglycosides
Therapeutic Actions and Indications
The aminoglycosides are bactericidal.
Where is Aminoglycosides best absorbed? Can it cause the placental barriers? What is the average half life of aminoglycosides?

Contraindication and Cautions


Allergy Hepatic disease Pre existing hearing loss Mycobacterial infection Myasthenia gravis and Parkinson's disease Lactation

Aminoglycosides
Adverse Effects
CNS Effects Renal Toxicity Bone Marrow Depletion GI effects Cardiac effects Hypersensitivity

Clinically Important Drug to Drug Interaction


Diuretics Neuromuscular blockers Penicillins, cephalosporins, carbenicillins

Nursing Consideration for Patients Receiving Aminoglycosides


1. 2. 3. 4. 5. 6. 7. 8. 9. 10.

Cephalosporins
Cephalosporins are the most frequently prescribed class of antibiotics They are structurally and pharmacologically related to penicillins Like penicillins, cephalosporins have a beta-lactam ring structure that interferes with the synthesis of bacterial cell wall The first agent cephalothin (cefalotin) was launched by Eli Lilly in 1964 Cephalosporins are used to treat a wide variety of bacterial infections, such as;
respiratory tract infections (pneumonia, tonsillitis, bronchitis), skin infections and urinary tract infections. They are also commonly used for surgical prophylaxis - prevention of bacterial infection before, during, and after surgery. They are sometimes given with other antibiotics to increase the spectrum of activity

Generation of Cephalosporins
First Generation Cephalosporins are moderate spectrum agents
Effective against gram negative aerobes They are effective for treating staphylococcal and streptococcal infections and therefore are alternatives for skin and soft-tissue infections, as well as for streptococcal pharyngitis. (PEcK)
Cefadroxil Cephalexin Cephaloridine Cephalothin Cephapirin Cefazolin Cephradine

Generation of Cephalosporins
Second Generations Cephalosporins - antibacterial spectrum is
broader than that of 1st generation Cephalosporins and includes some gram negative pathogens They are useful agents for treating upper and lower respiratory tract infections and sinusitis

H.E.N.PeC.K
The second generation drugs are less effective against gram positive bacteria
Cefaclor Cefmetazole Cefonicid Cefotetan Cefoxitin Cefprozil Cefuroxime

Generation of Cephalosporins
Third Generations Cephalosporins HENPeCKS The parenteral third generation Cephalosporins (ceftriaxone and cefotaxime) have excellent activity against most strains of Streptococcus pneumonia, including the vast majority of those with intermediate and high level resistance to penicillin The third generation Cephalosporins are:
Cefdinir Cefoperazone Cefotaxime Cefpodoxime Ceftazidime Ceftibuten Ceftozoxime Ceftriaxone

Generation of Cephalosporins
Fourth Generations Cephalosporins 4th generation Cephalosporins are extended spectrum agents with similar activity against gram-positive organisms as first generation Cephalosporins. Many can cross blood brain barrier and are effective in meningitis.

Therapeutic Action and Indications


Bacteriostatic and Bactericidal
Where it is best absorbed? What are the sign of GI adverse reaction? Clinically Important Drug to Drug Interaction
What out for nephrotoxicity if used together with aminoglycosides Patient receiving anticoagulants Avoid drinking alcohol after 72 hours of taking Cephalosporins

Nursing Considerations for Patients Receiving Cephalosporins


1. 2. 3. 4. 5. 6. 7. 8. 9. 10.

Fluoroquinolones
Are a relatively new synthetic class of antibiotics with a broad spectrum of activity. The fluoroquinolones enter the bacterial cell by passive diffusion through channels in the cell membrane. Once inside, they interfere with the action of DNA enzymes necessary for the growth and reproduction of the bacteria. This leads to cell death because the bacterial DNA is damaged and the cell cannot be maintained.

Drugs

Contraindications

Ketolides, Macrolides, Lincosamides, Monobactam

Ketolides, Macrolides, Lincosamides, Monobactam

Penicillins and Penicillinase

Penicillins and Penicillinase

Penicillins and Penicillinase

Sulfonamides

Tetracycline

Antimycobacterial

Antimycobacterial

PRINCIPAL EVENTS INVOLVED IN REPLICATION


Adsorption The first step in infection of a cell is attachment to the cell surface. Attachment is via ionic interactions which are temperatureindependent. The viral attachment protein recognizes specific receptors, which may be protein, carbohydrate or lipid, on the outside of the cell. Cells without the appropriate receptors are not susceptible to the virus. Penetration The virus enters the cell in a variety of ways according to the nature of the virus. Un-coating Nucleic acid has to be sufficiently uncoated that virus replication can begin at this stage. When the nucleic acid is uncoated, infectious virus particles cannot be recovered from the cell - this is the start of the ECLIPSE phase - which lasts until new infectious virus are made.

Synthesis of viral nucleic acid and protein Many strategies are used, some will be discussed in later chapters. Assembly/maturation New virus particles are assembled. There may be a maturation step that follows the initial assembly process. Release Virus may be released due to cell lysis, or, if enveloped, may bud from the cell. Budding viruses (figures 3 and 4) do not necessarily kill the cell. Thus, some budding viruses may be able to set up persistent infections. Not all released viral particles are infectious. The ratio of non-infectious to infectious particles varies with the virus and the growth conditions.

HIV Replication
Steps in the HIV Replication Cycle
Fusion of the HIV cell to the host cell surface. HIV RNA, reverse transcriptase, integrates, and other viral proteins enter the host cell. Viral DNA is formed by reverse transcription. Viral DNA is transported across the nucleus and integrates into the host DNA. New viral RNA is used as genomic RNA and to make viral proteins. New viral RNA and proteins move to cell surface and a new, immature, HIV virus forms. The virus matures by protease releasing individual HIV proteins.

CD4 a large glycoprotein that is found on the surface of helper T cells, regulatory T cells, monocytes, and
dendritic cells. Its natural function is as a coreceptor that assists the T cell receptor (TCR) to activate its T cell following an interaction with an antigen presenting cell. CD4 is a primary receptor used by HIV1 to gain entry into host T cells. Coreceptor (CCR5 or CXCR4) protein molecules on the surface of lymphocytes or monocytes that bind to the gp120 protein of HIV and facilitate, usually with CD4, entry of viral nucleic acid and proteins into the cell. DNA (deoxyribonucleic acid) is a nucleic acid that contains the molecular basis of heredity for all known living organisms and some viruses and is found in the nuclei and mitochondria of eukaryotes. Chemically DNA consists of two polymer strands of units called nucleotides made up of one of four possible bases plus sugar and phosphate groups. The polymers are joined at the bases by hydrogen bonds to form a double helix structure. Fusion of virus and cell membranes a merging of cell and virus membranes that permits HIV proteins and nucleic acids to enter the host cell. Genomic RNA the nucleic acid that contains all of the hereditary information of a virus, and is found in a mature virion. gp120 an HIV glycoprotein having a molecular weight of 120 that protrudes from the outer surface of the virion. This glycoprotein binds to a CD4 receptor on a T cell to facilitate entry of viral nucleic acid and proteins into the cell. HIV (human immunodeficiency virus) is a lentivirus and a member of the retrovirus family. HIV infects and destroys helper T cells of the immune system causing a marked reduction in their numbers. Loss of CD4 cells leads to generalized failure of the immune system and susceptibility to life threatening opportunistic infections.

Integrase An enzyme found in retroviruses including HIV that permits the viral DNA to be integrated into the DNA of the infected cell. Preintegration complex (PIC) It is composed of viral RNA and proteins (nucleocapsid, p6, Vpr, integrase, and matrix) as well as some host proteins. It functions to reverse transcribe genomic RNA into double stranded DNA prior to integration into the host genomic DNA. Protease an enzyme that hydrolyzes or cuts proteins and is important in the final steps of HIV maturation. Nucleus a membrane enclosed cellular organelle of eukaryotes that functions to contain the genomic DNA and to regulate gene expression. Reverse transcriptase an enzyme found in HIV that creates double stranded DNA using viral RNA as a template and host tRNA as primers. RNA (ribonucleic acid) a nucleic acid that differs from DNA in that it contains ribose and uracil as structural components. RNA virus a virus that uses RNA as its genetic material and belongs to either Group III, IV, or V of the Baltimore Classification System of Viruses. HIV belongs to Group III, double stranded RNA viruses. Virion a single and complete extracellular infective form of a virus that consists of an RNA or DNA core with a protein coat or "envelope".

A female Anopheles mosquito carrying malaria-causing parasites feeds on a human and injects the parasites in the form of sporozoites into the bloodstream. The sporozoites travel to the liver and invade liver cells. Over 5-16 days*, the sporozoites grow, divide, and produce tens of thousands of haploid forms, called merozoites, per liver cell. Some malaria parasite species remain dormant for extended periods in the liver, causing relapses weeks or months later. The merozoites exit the liver cells and re-enter the bloodstream, beginning a cycle of invasion of red blood cells, asexual replication, and release of newly formed merozoites from the red blood cells repeatedly over 1-3 days*. This multiplication can result in thousands of parasite-infected cells in the host bloodstream, leading to illness and complications of malaria that can last for months if not treated.

Some of the merozoite-infected blood cells leave the cycle of asexual multiplication. Instead of replicating, the merozoites in these cells develop into sexual forms of the parasite, called male and female gametocytes, that circulate in the bloodstream. When a mosquito bites an infected human, it ingests the gametocytes. In the mosquito gut, the infected human blood cells burst, releasing the gametocytes, which develop further into mature sex cells called gametes. Male and female gametes fuse to form diploid zygotes, which develop into actively moving ookinetes that burrow into the mosquito midgut wall and form oocysts. Growth and division of each oocyst produces thousands of active haploid forms called sporozoites. After 8-15 days*, the oocyst bursts, releasing sporozoites into the body cavity of the mosquito, from which they travel to and invade the mosquito salivary glands. The cycle of human infection re-starts when the mosquito takes a blood meal, injecting the sporozoites from its salivary glands into the human bloodstream .

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