2009B04 Describe the effect of obesity on pharmacokinetics and the potential
clinical implications, providing relevant examples.

 

List:

·     Obesity

·     Absorption

·     Distribution

·     Metabolism

·     Excretion

·     Modelling

 

Obesity:

Definition

BMI >30kg/m2 body surface area

Changes

·  ↑Fat mass

o Accounts for 60-80% excess

o  -> Chest wall compression, diaphragm displacement

·  ↑Fat-free mass

o Accounts for 20-40% excess. Rarely >70kg in women, >100kg in men

o ->↑Metabolic rate (BMR), ↑blood volume, ↑cardiac output (CO)

·  ↑Visceral fat

o ↑Inflammatory cytokines (e.g. TNFα, IL-1, IL-6 in metabolic syndrome)

·  Comorbid disease

o Much more likely with central obesity

 

Absorption:

Oral

·  Delayed gastric emptying -> slow onset

o e.g. ineffective oral pre-medication

Inhalational

·  ↑VA:FRC -> ↑rate of rise FA/FI

o ↑Metabolic rate -> ↑VCO2 -> ↑VA awake

(but ↓VA under GA due to poor compliance)

o Diaphragm compression -> ↓↓FRC (e.g. ↓25% when erect at BMI 35)

(worse supine, even worse under GA)

Intramuscular

·  Risk of subcut injection -> ↓onset, risk of dose stacking

 

Distribution:

Circulation

·  ↑CO ↑lean mass

o ↑Rate of drug distribution

o ↓Peak plasma [propofol] after bolus -> risk of awareness

o ↓Rate of rise FA/FI volatile anaesthetic (partly offsets resp changes)

·  ↑Blood volume

o ↑Central VD -> ↓Plasma concentration after loading dose

o Risk of awareness post-induction

Plasma proteins

·  Altered profile in metabolic syndrome

·  ↓Albumin -> ↑unbound % of acidic drugs -> toxicity if low HER (e.g. phenytoin)

·  ↑AAG -> ↓unbound % basic drugs (e.g. morphine)

Tissues

*Dosing by total body weight may cause toxicity*

·  ↑Total body water

o ↑VD water-soluble drug -> resistance to effect of muscle relaxants

o Note overdose likely if loading dose calculated with total body weight

·  ↑Muscle

o ↑Time constant -> slow emergence from volatile anaesthetic

o ↑Time to emergence from volatile anaesthetic

·  ↑Fat

o ↑VD fat-soluble drugs -> ↑t1/2β (e.g. fentanyl)

o ↑Time constant -> slow emergence only if very long volatile anaesthetic

 

Metabolism:

Hepatic

·  Significant impairment only if NAFLD-induced cirrhosis

·  Phase 1: variable effect on CYP450 enzymes

o ↓3A4 (most drugs)

o ↑2E1 (volatiles)

·  Phase 2: ↑activity

Other

·  ↑Plasma cholinesterase -> ↑resistance to suxamethonium
(hence dosing according to TBW)

 

Excretion:

Urine

·  ↑Renal blood flow ↑lean mass

o ↑Excretion of small and/or hydrophilic drugs and metabolites

o e.g. morphine 6 glucuronide

Bile

·  Unaffected by simple obesity

Lung

·  ↑VA:FRC -> ↑rate of fall FA/FA0 (causes as above)

 

Modelling:

Marsh TCI

·  Entry of total body weight inappropriate

o ↑Dose -> toxicity (i.e. hypotension)

Schnider TCI

·  Poor estimate of lean mass (James equation)

o Paradoxical ↓infusion rate at BMI >42 in men, >35 in women

o Risk of awareness

 

 

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