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27 Cards in this Set

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Pharmacokinetics...

How the body affects the drug.

Pharmacodynamics...

How the drug affects the body...

What is a drug?

A substance used in the...


- diagnosis, treatment or prevention of a disease.


- or as a component of a medication.

Why is 'small' advantageous?

Quicker access into the body.




Reach target (chemically sensitive site) sooner.




Longer to excrete.

What is an agonist?

Activates receptors and elicits a response...


- Drug


- Hormone


- Neurotransmitter


- Signaling molecule

What is an antagonist?

Prevent (block) effect of agonist...


- Competitive.


- Non-competitive.

What is affinity?

How well the drug binds to the receptor...


- Depends on the concentration of the drug.


- Removal depends on how well it was bound in the first place.


- If we know how much drug we need for the receptor site, we know what kind of dose we need.

Pharmacokinetics; 4 Stages?

1. Absorption


2. Distribution


3. Metabolism


4. Excretion

Routes of administration?

- Oral (po)


- Inhaled (inh)


- Topical (top)


- Sub lingual (s/l)


- Rectal (pr)


- Parenteral (bypassing digestive system ((injection)))

What is the half life?

The time it takes for the drug in the body to drop to half the original.

Where does drug metabolism occur?

Liver

Where does drug excretion occur?

Kidneys

Opiates - Class effect (CNS system)

- Analgesia


- Euphoria (mew receptors)


- Respiratory depression (commonest cause of death)


- Cough suppression


- Pin point pupils (mew & k receptors)


- Nausea and vomiting (SE)

Opiates - Class effect (elsewhere)

- Constipation (GI system)


- Bronchospasm


- Hypotension


- Local itchiness

What is drug tolerance?

Receptor desensitisation, therefore increasing dose to get same pharmacological effect.

What is dependence?

Physical, physiological dependence on drug - withdrawal symptoms.


- Signs of aggression


- Irritability


- Diarrhoea


- Weight loss




Symptoms can last for weeks.

WHO Pain relief ladder

Non-opioid


- Paracetamol


Adjuvant


- NSAIDs (ibruprofen, diclofenac)


Opioid (mild)


- Codeine


- Dihydrocodeine


- Tramadol


Opioid (mod-severe)


- Morphine

What is a TTO?

TTO = To Take Out


It is the supply of medication in addition to what the patient already possesses at home that the patient is issued with upon discharge from hospital.

What does a GP need from a discharge letter?

Relevant information regarding new medication; dose, time, administration.


Reason for starting patient on TTO medication.


Whether the hospital prescribed prophylaxes should be continued.

Where do you obtain a reliable drug history if the patient is confused?

- Patient's partner/carer


- Patient's own medicines


- GP surgery


- GP referral letter


- Previous discharge prescriptions


- Care home records


- Community pharmacy

Salbutamol

-B2-receptor agonist.


-Bronchodilation; Relaxes uterine and smooth muscle.


-Used for asthma.


-Decrease in calcium-mediated contraction in bronchioles.


-Increases cAMP which activates protein kinase which inhibits myosin light chain kinase (the mediator of contraction).

Atenolol

- B1 antagonist


- Reduces BP in hypertensive patients by decreasing cardiac output.


- Block of the action of endogenous and exogenous agonists on B1-receptors.


- Used in hypertension and angina.


- Can cause bronchoconstriction in asthma.

Ibuprofen

NSAID


- Reduces inflammation


- Analgesic for inflammatory pain


- Antipyretic (reduces raised temperature)


- Reversible inhibition of COX-1, weak inhibition of COX-2.


- GI disturbances.

Aspirin


NSAID


- Reduces inflammation.


- Analgesic for inflammatory pain.


- Antipyretic (reduces raised temperature).


- Inhibits platelet aggregation.


- Irreversible acetylation of cyclo-oxygenases; weakly COX-1 selective.

Aspirin Special Points


- Should not be used in children.


- Can cause increased effect of warfarin resulting in bleeding.


- Should not be used for gout because it reduces urate excretion and interferes with the action of uricosuric agents.

Paracetamol

- Analgesic and antipyretic (i.e. reduces raised temperature).


- Has little anti-inflammatory action.


- Inhibition of COX-1, COX-2 and also the recently identified COX-3 which occurs predominantly in the CNS.


- Mild to moderate pain, especially headache.

Methotrexate


- Has marked anti-inflammatory action in rheumatoid disease.


- Cytotoxic in the larger doses used to treat cancer.


- First choice for RA.


- Also used in psoriasis, ankylosing spondylitis, polymyositis and vasculitis.


- MTX is also an anti-cancer agent.


- GI disturbances, liver toxicity, bone marrow depression.