Pharmacology Flashcards
Define pharmacology
The study of the effects of the drug
Define pharmokinetics (PK)
How the body affects the drug: Absorption, Distribution, Metabolism and Excretion (ADME)
Define pharmacodynamics (PD)
How the drug affects the body
What are the 4 main actions of pharmacokinetics
- ) Absorption
- ) Distribution
- ) Metabolism
- ) Excretion
Describe the process of absorption in pharmacokinetics
- Absorption = the process of transfer from site of administration into the systemic circulation
- Routes of transmission: oral/intramuscular/topical/inhalational/intravenous/sublingual/intra arterial
- To be absorbed the drug needs to pass through one membrane minimum
- They do this via:
- passive diffusion through the lipid layer
- diffusion through pores or ion channels
- pinocytosis
- carrier mediated process (e.g. ATP-binding cassette)
Give an example of absorption within pharmacokinetics
- E.g oral absorption
- Advantages: good due to large SA and high blood flow in the small intestines
- Disadvantages: drugs can be metabolised, so less efficient
What are the main factors that affect the speed of oral absorption?
- ) First pass metabolism: drugs need to get through the intestinal lumen, intestinal wall, liver and lungs
- ) Drug structure and formulation
- ) Gastric emptying
Describe the process of distribution in pharmacokinetics
Distribution = the process by which the drug is transferred from general circulation to tissues, occurring via passive diffusion across cell membranes
Give an example of distribution in pharmacokinetics
IV drugs: initially you have a high plasma concentration. Drugs will quickly enter well perfused tissue and then the drug will enter the less well perfused tissues and lower the plasma concentration
What are some important points on distribution in pharmacokinetics?
- Remember most drugs bind to plasma/tissue proteins. Thus, by binding you will lower the ‘free’ concentration of the drug
- Distribution is important as it determines the total amount of drug that has to be administered to produce a particular plasma concentration
How do you measure distribution of a drug?
Vd: the total amount of drug in body/plasma concentration
What does the rate of distribution for water soluble drugs depend on?
The rate of passage across membranes
What does the rate of distribution for lipid soluble drugs depend on?
The blood flow to tissues that accumulate the drug
Define clearance
The volume of blood or plasma cleared of the drug per unit time
Define metabolism in pharmacokinetics
Metabolism = the process where lipid soluble drugs are converted into water soluble molecules
What are the names of the two reactions involved in metabolism in pharmacokinetics?
- ) Phase 1
2. ) Phase 2
Describe a phase 1 reaction in metabolism
- The drug is transformed into a more polar metabolite
- This is done by adding a functional group
- Common example is oxidation (catalysed by p450 enzymes)
Describe what P450 enzymes are
- They are isoenzymes
- They are present in the smooth endoplasmic reticulum
- Grapefruit inhibits them
- Smoking induces them
Describe a phase 2 reaction in metabolism
- Involves the formation of a covalent bond between: the drug, and its phase 1 metabolite
- It is an endogenous substrate
- End result: a less active drug that can be excreted by the kidneys
Define excretion
Drugs and metabolites are excreted in:
- fluids: urine and sweat
- solids: faeces
- gases
Define antibiotic
Antibiotic = an antibacterial drug. Work by binding a target site on bacteria. Semi-synthetic derived of antibiotics are ‘antimicrobials’
What does the class of ‘antimicrobials’ include
- antifungal
- antibacterial
- anthelminthic
- antiprotozoal
- antivirals
Define the key mechanisms of actions of antibiotics (what do they block)
- ) Inhibit protein synthesis
- ) Inhibit cell wall synthesis: e.g. beta lactams disrupt the peptidoglycan production by binding covalently to the PBPs-> results in lysis
- ) Inhibit nucleic acid synthesis
- ) Anti-metabolites
- ) Inhibit membrane function
Give 4 examples of antibiotics that inhibit cell wall synthesis
- ) Penicillin: Penicillin V or Amoxicillin
- ) Cephalosporins: cephalexin or cefotaxime (use is person has penicillin allergy)
- ) Carbapenems: meropenem or entapenem
- ) monobactams: aztreonam
- note: all beta-lactams