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Locomotor & Exercise > Exercise-Drug Interactions > Flashcards

Exercise-Drug Interactions Flashcards

1
Q

Vasoconstriction is mediated by

A

alpha 1 receptors

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2
Q

Vasodilation is mediated by

A

beta 2 receptors

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3
Q

The effects of redistributed blood flow in exercise affect absorption

A

based on route of administration

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4
Q

The effects of redistributed blood flow in exercise affect distribution by

A

increased muscle and skin blood flow

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5
Q

The effects of redistributed blood flow in exercise affect metabolism by

A

decreased hepatic blood flow

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6
Q

The effects of redistributed blood flow in exercise affect excretion by

A

Decreased renal blood flow

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7
Q

What is the risk of exercise in insulin-dependent diabetes?

A

plasma insulin can rise during exercise and tf glucose control may be dysregulated

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8
Q

What are mechanisms of exercise-induced hypoglycaemia?

A

Accelerated insulin absorption from sites near exercising muscles; exercise-mediated enhancement of insulin action; lack of decline in insulin secretion during exercise (ie secrete insulin during exercise)

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9
Q

What are mechanisms of exercise-induced hyperglycaemia?

A

Excessive CHO supplementation; too large a reduction in insulin dose pre-exercise

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10
Q

What is the risk in using transdermal glyceryl trinitrate in exercise (or hot environments)?

A

plasma levels of GTN can be increased by the associated: inc skin blood flow, inc kinetic energy of drugs with inc skin temperature, inc hydration which improves absorption of drugs with diffusion rate-limited absorption

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11
Q

What are the implications of increased transdermal absorption of GTN in exercise?

A

may be beneficial by further minimizing risk of exercise-induced angina; potential for vasodilation in skin and exercising muscle to cause excessive hypotension and divert coronary blood flow esp in hot environments - can get precipitous hypotension (severely low BP)

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12
Q

Salbutamol

A

works on B2 receptors in airways to cause bronchodilation

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13
Q

What are the consequences of taking salbutamol prior to or during exercise?

A

plasma levels can become increased due to the increased respiratory rate, increased pulmonary blood flow, and increased epithelial permeability

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14
Q

What are the implications of increased absorption of salbutamol in exercise?

A

May provide benefit by minimizing exercise-induced asthma; despite higher bioavailability though, bronchodilator effects are less prolonged - it wears off quicker so dosing needs to be more frequent

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15
Q

How does exercise impact the gut?

A

inhibits gastric emptying; increases intestinal motility to reduce transit time; decreases splanchnic blood flow

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16
Q

How does inhibition of gastric emptying in exercise affect drugs in the gut?

A

reduces drug delivery to the SI tf decreasing absorption; adaptation occurs in trained athletes

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17
Q

How does increased intestinal motility in exercise affect drugs in the gut?

A

reduced transit time means less time for absorption of lipophilic drugs

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18
Q

How does decreased splanchnic blood flow in exercise affect drugs in the gut?

A

more time for absorption of drugs where diffusion is the rate limiting step

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19
Q

What are the risks of warfarin in exercise?

A

Increased bruising and decreased INR (clotting time)

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20
Q

How is INR purportedly shortened by exercise?

A

Warfarin is more bound to plasma albumin because of fluid loss; may be an increase in metabolism of the drug with training; in both, get decreased free warfarin = more clotting/decreased INR

21
Q

What is the implication of decreased INR with exercise?

A

Increased clotting and risk of thrombosis

22
Q

How does exercise affect levels of digoxin in the body?

A

Digoxin has a high volume distribution tf goes into muscle, not much in plasma; in exercise, there is reduced plasma digoxin but increased distribution and binding to skeletal muscle

23
Q

What is the mechanism of decreased plasma levels of digoxin in exercise?

A

Redistribution due to increased binding to skeletal muscle tf not much is left in plasma

24
Q

What are the implications of decreased plasma digoxin in exercise?

A

Digoxin is used to maintain contractility or control HR - can dysregulate this, lead to arrythmias

25
Q

How does exercise affect propranalol (non-selective b-blocker)?

A

increased in plasma due to reduced hepatic clearance (metabolism)

26
Q

How does exercise affect atenolol (selective B1 b-blocker)?

A

increased in plasma due to reduced renal clearance (excretion)

27
Q

How does exercise affect carvedilol (mixed B-blocker and A-antagonist)?

A

unchanged

28
Q

What are the implications of increased plasma levels of beta-blockers with exercise?

A

Increased risk of exercise-limiting adverse effects eg not being able to increase HR, off-target (not on heart) B2-mediated bronchoconstriction can block B2-mediated bronchodilation, reduced blood flow to skeletal muscle through B2 vasodilation, fatigue

29
Q

What advantage do diuretics confer in sport?

A

dilution of urine to mask banned drugs; fluid loss leading to weight loss to meet a lower weight class

30
Q

Clinically, diuretics are used for

A

oedema, hypertension, cardiac failure

31
Q

What are the disadvantages and adverse effects of diuretics in sport?

A

dehydration; hypokalaemia due to inhibition of Na+ reabsorption

32
Q

What is the role of B1 receptors in exercise?

A

SNS activation increases NA & A –> cardiac pacemaker tissue to +HR; cardiac muscle to +SV; adipose tissue to +lipolysis

33
Q

What is the role of B2 receptors in exercise?

A

SNS activation increases NA & A –> airway smooth muscle to bronchodilate; blood vessels in skeletal muscle and skin to increase blood flow; skeletal muscle to increase growth, speed of contraction, tremor; liver to promote glycolysis

34
Q

Clinically, B1 antagonists are used for

A

hypertension; reducing HR, SV, CO, BP by blocking cardiac B1 receptors

35
Q

B1 antagonists

A

propranolol, atenolol

36
Q

What is the advantage of B1 antagonist use in sport?

A

reduction of HR and stress; reduce tremor in hands and bodies in precision accuracy sports

37
Q

What are the disadvantage of B! antagonists in sport?

A

lowered BP and decreased HR so can’t increase to meet demand; reflex vasoC via A1rs; nonselective block of B2r vasoD of skeletal/skin blood vessels; fatigue, decreased performance in endurance events

38
Q

What is the advantage of B2 agonist use in sport?

A

systemic administration or high dose inhalation: increased skeletal muscle blood flow to +O2 supply and remove lactic acid , reducing fatigue; anabolic effects of increasing muscle mass and strength; catabolic effects to reduce body fat to meet weight category

39
Q

What are the adverse effects of B2 agonists in sport?

A

tachycardia via nonselective activation of cardiac B1aRs; muscle tremor via activation of skeletal muscle B2aRs

40
Q

What is the advantage of glucocorticosteroids in sport?

A

Anti-inflammatory use can mask pain

41
Q

What are the disadvantages of glucocorticosteroid use in sport?

A

damage to tissues before full recovery; chronic use can precipitiate cushings-like syndorme - osteoporosis, growth suppression in children, skin fragility, increased infections

42
Q

What is the status of glucocorticosteroid use in sport?

A

topical and inhalation are approved; abbreviated TUE for intra-articular; banned systemically

43
Q

What is the advantage of anabolic steroid use in sport?

A

increased muscle strength by encouraging new growth; allows for longer, harder training

44
Q

What are the disadvantages of anabolic steroid use in sport?

A

high BP; decreased good/increased bad cholesterol; jaundice & liver damage; mood swings, depression, aggression; acne; male baldness, breast development, infertility; female hair growth on face and body, deepened voice, menstrual disruption, possible infertility

45
Q

What is the advantage of growth hormone use in sport?

A

Reduced fat mass, increased lean mass, increased bone density

46
Q

What are the adverse effects of GH use in sport?

A

joint pain, increased diabetes risk, acromegaly

47
Q

AOD9604

A

(unproven) Anti-obesity drug 9604 aka Lipotropin - designed to be catabolic to break down fat but not anabolic (doesn’t stimulate IGF-1)

48
Q

What is the advantage of AOD9604 use in sport?

A

unproven as anti-obesity; under preclinical trials for repair of cartilage, muscle, and joint disorders eg OA

49
Q

What are the potential adverse effects of AOD9604 use in sport?

A

headache, chest tightness, palpitations, euphoria; long-term effects are not known

Locomotor & Exercise (11 decks)

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