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WEEK 5:
ADME 1
| Question | Answer |
|---|---|
| ADME | absorption, distribution, metabolism, excretion |
| TDM | therapeutic drug monitoring |
| pharmacokinetics | how the body processes drug (ADME) |
| pharmacodynamics | how drug affect body |
| routes of administration | local and systemic |
| local administration (5) | topical, rectal + vaginal, dermal, eyes + ears + nose, inhalation |
| systemic administration | parenteral + enteral |
| parenteral (7) | IV, IM, subcutaneous, intraarticular, intrathecal, intravitreal, inhalation |
| enteral (3) | oral, sublingual + buccal, rectal + vaginal |
| bioavailability | shows fraction of orally administered drug that reaches systemic circulation as an intact drug |
| intravenous route bioavailability + characteristics | (bioavailability = 100%) (characteristics = most rapid onset) |
| intramuscular route bioavailability + characteristics | (bioavailability = 75 to ≥ 100%) (characteristics = large volume feasible but painful) |
| subcutaneous route bioavailability + characteristics | (bioavailability = 75 to ≥ 100%) (characteristics = smaller volume than IV + painful) |
| oral route bioavailability + characteristics | (bioavailability = 5 to ≥ 100%) (characteristics = most convenient with significant 1st pass) |
| rectal route bioavailability + characteristics | (biodiversity = 30 to ≥ 100%) (characteristics = less 1st pass effect than oral) |
| inhalation route bioavailability + characteristics | (biodiversity = 5 to ≥ 100%) (characteristics =often very rapid onset) |
| transdermal route bioavailability + characteristics | (biodiversity = 80 to ≥ 100%) (characteristics = slow absorption, lack of 1st pass, prolonged duration of action) |
| types of oral administrations | solutions, suspensions, tablets, capsules |
| describe oral administrations | convenient + economical, allows interpatient variation, variable bioavailability, requires patient cooperation, can be affected by food + other medications |
| first pass metabolism | drug metabolism (broken down) before drug enters systemic circulation, reducing bioavailability + therapeutic response |
| how can you bypass first pass metabolism | IV route, sublingual route |
| example of drug with a high first pass metabolism | salbutamol |
| drugs with a high first metabolism should be given how? | at higher doses more frequently |
| sublingual (SL) drugs | drugs diffuse into blood through mucous tissue under tongue, no first past, faster absorption, quick termination eg GTN or fentanyl |
| buccal drugs | dosage placed between gums + inner lining of cheek eg prochlorperazine |
| rectal route advantages | can be taken for local effect when oral medication isn't available or if patient is vomiting, can have a significant amount in blood |
| rectal route disadvantages | inconvenient, unpredictable absorption, localised irritation, cultural issues |
| intravireal parenteral route | through the eye eg bevacizumab in wet AMD |
| intradermal parenteral route | injection into dermis eg mantoux test for tuberculosis |
| intracavernous parenteral route | injection into base of penis |
| intramuscular parenteral route | vaccines eg depot antipsychotics |
| intraarticular parenteral route | injection in joints eg osteoarthritis |
| epidural parenteral route | injection into epidural space |
| intravenous parenteral route | medication given directly into vein |
| what are some drug administration considerations | ease of administration (eg is the patient compliant + does it require staff help), kinetics of drug (eg how fast and long it works), target organ (local or systemic effect), side effects (therapeutic range) |
| PO | oral |
| IM | intramuscular |
| IV | intravenous |
| SC | subcutaneous |
| Neb | nebuliser |
| OD | once daily |
| EOD | every other day |
| BD/BID | twice daily |
| TDS | three times a day |
| QDS/QID | four times a day |
| PRN | as required |
| examples of drugs given via intravenous route | lidocaine (antiarrhythmic), co-amoxiclav (antibiotic therapy), suxamethonium (surgery + intubation), phenytoin (status epilepticus), furosemide (pulmonary oedema), thrombolytic drug (stroke/ MI), theophylline (status asthmaticus) |
| advantages of intravenous route | directly in bloodstream, rapid effects so can adjust drug dose if needed, can use large volumes and irritating substances as long as its diluted |
| disadvantages of intravenous route | increased risk of adverse effects (100% bioavailability so large volumes can be toxic), risk of air embolism (air bubble), can't use oily solution/insoluble substances, requires IV access, painful |
| describe the graph for intravenous route | straight diagonal line going down |
| examples of drugs given via subcutaneous route | insulin (diabetes) + low molecular weight heparin (enoxaparin- prevents deep-vein thrombosis) |
| advantages of subcutaneous route | fast absorption if drug is dissolved in aqueous solution, slow + gradual release for long-lasting effect, can use some insoluble suspensions/ solid pellets |
| disadvantage of subcutaneous route | can't use large volumes, possible pain or necrosis from irritating substances |
| examples of drugs given via intramuscular route and can be given via IV | benzylpenicillin (antibiotic therapy), ceftriaxone (pneumonia), gentamicin (endocarditis) |
| advantages of intramuscular route | fast absorption if drug is dissolved in aqueous solution, slow + gradual release for long-lasting effect, can use moderate volumes, oily + irritating substances, rapid onset of action, high bioavailability |
| disadvantages of intramuscular route | painful + risk of injection at wrong site causing nerve damage |
| examples of topical route | eye drops, nasal sprays, dermatological creams |
| examples of transdermal route | patches |
| examples of inhalation route | asthma drugs, general anaesthetics |
| bolus injection | single large dose of a drug which produces rapid, high concentrations, useful for patient who is fluid restricted |
| stat dose | immediate dose |
| therapeutic range | range of drug dosages that provide effective treatment |
| drugs with a narrow therapeutic range (NTI) | drugs where small differences in dose/blood concentration can lead to serious therapeutic failures or adverse reactions |
| examples of drugs with a narrow therapeutic range (NTI) | lithium, warfarin, digoxin, phenytoin, theophylline, ciclosporin/tacrolimus, gentamicin |
| intrathecal parenteral route | injection in spinal canal eg chemotherapy or spinal anaesthesia |
| types of injections | intramuscular, subcutaneous, intravenous, intradermal |
| angle for intramuscular injection | 90 degrees |
| angle for subcutaneous injection | 45 degrees |
| angle for intravenous injection | 25 degrees |
| angle for intradermal injection | 10/15 degrees |
| lidocaine | taken via IV, used for antiarrhythmic (treating irregular heart rhythms) |
| co-amoxiclav | taken via IV, used for antibiotic therapy |
| suxamethonium | taken via IV, used for surgery + intubation (tube down nose/mouth into trachea to open airway) |
| phenytoin | taken via IV, used for status epilepticus (continuous seizures) |
| furosemide | taken via IV, used for pulmonary oedema (excess watery fluid in lungs) |
| thrombolytic drugs | taken via IV, used for stroke (MI) |
| theophylline | taken via IV, used for status asthmaticus (severe asthma attack) |
| examples of drugs that can be given via intramuscular route | benzylpenicillin (antibiotic therapy), ceftriaxone (pneumonia), gentamicin (endocarditis), influenza vaccine, sex hormone eg testosterone, vitamin B12 |
| benzylpenicillin | drug given via IM/IV for antibiotic therapy |
| ceftriaxone | drug given via IM/IV for pneumonia |
| gentamicin | drug given via IM/IV for endocarditis (inflammation of endocardium- the inner lining of the heart) |
| therapeutic range | drug concentration in blood that provides effective treatment |
| reasons why there may be no simple relationship between plasma drug level and therapeutic response | active metabolites, receptor sensitivity + tissue distribution, tolerance + pharmacodynamic factors |
| active metabolites | some drugs are metabolised into active forms that cause the therapeutic effect |
| receptor sensitivity + tissue distribution | drug needs to bind to receptor in order to work but the amount in plasma might be different from the amount reaching receptor + amount of receptors + sensitivity vary |
| tolerance + pharmacodynamic factors | overtime the body can become less responsive to a drug even at same plasma concentrations so higher doses are needed for the therapeutic effect |
Created by:
kablooey
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