Locomotor Drugs Actions

Question 1

Simple analgesics

Answer 1

inhibit COX enzyme. Prevent arachidonic acid from being converted to prostaglandins. Central action. No anti inflammatory effect. Mechanism of action unclear

Question 2

Opioid analgesics

Answer 2

Agonists on mu opioid receptors at spinal cord, thalamus, midbrain, medulla. Also cause euphoria, peace, contentment, calm. Presynaptic effects: inhibits NT release by reducing influx of Calcium. Post synaptic: inhibits post-stn NT by activating K+ channels leading to hyperpolarisation.

Question 3

NSAIDs

Answer 3

inhibit COX isoforms to reduce PG formation which reduces pain sensitivity and ongoing inflammation. All but aspirin bind reversibly

Question 4

Neuropathic/ anti-epileptic

Answer 4

blocks voltage gated NA+ channels in recovery phase, keeping the channels closed and resistant to activation for a longer time period than usual

Question 5

Anti-migraine

Answer 5

5HT1 agonists that cause vasoconstriction

Question 6

Nitrates

Answer 6

broken down in vascular tissues to release NO or nitrosothiol. Vasodilation. Reduce BP. Reduce venous return to heart. All these reduce mismatch between O2 demand and supply to heart.

Question 7

Local anaesthetics (-caine)

Answer 7

blocks sodium channels to prevent membrane depolarisation

Question 8

Local anaesthetics with adrenaline

Answer 8

Adrenaline causes vasoconstriction and so prolongs the effect of the LA

Question 9

Corticosteroids

Answer 9

Analogues of endogenous glucocorticoids. bind to intracellular receptors to alter translation of DNA. Macrophages and T cells are key cell targets in inflammation. In bone; reduce osteoblast differentiation, increase osteoclast activity, decrease calcium absorption

Question 10

Methotrexate

Answer 10

immunosupressant, blocks DNa synthesis in proliferating cells by binding with and blocking the action of folic acid reductase

Question 11

Sulfasalazine

Answer 11

anti-inflammatory, systemic immunosuppressant activity

Question 12

Cytokine inhibitor

Answer 12

cytokine inhibitor, blocks pro-inflamm action of TNA-a. Monoclonal antibody. Expensive

Question 13

Glycosaminoglycan anticoagulants

Answer 13

potentiates activity of antithrombin 3, interferes with coagulation cascade

Question 14

Bisphosphates

Answer 14

decrease osteoclast activity, reduce hip fracture incidence and greatly reduce risk of spinal fractures

Question 15

Oestrogen/ HRT

Answer 15

interacts with intracellular receptors to inhibit bone resorption by osteoclasts. Reduce hip an spinal fractures in post-menopausal women. moderately effective, not as effective as bisphosphonates. Rarely used now.

Question 16

Calcitonin

Answer 16

inhibits osteoclasts, slows bone loss, increases spinal bone density. It is a protein therefore must be IV or nasal spray.

Question 17

PTH

Answer 17

modified forms (teriparatide 1-34 fragment) stimulate bone formation by osteoblasts and significantly increase BMD. 70% reduction in vertebral fractures and 50% non vertebral. Injection as also a protein

Question 18

Oestrogen receptor modulator

Answer 18

oestrogen receptor agonist at some tissues (bone) and antagonist at others (breast)

Question 19

Calcium supplements

Answer 19

key mineral in bone formation, and for heart muscles and nerves,

Question 20

Vitamin D

Answer 20

needed for body to absorb calcium