Pharmacology

Question 1

Agonists

Answer 1

Drugs that mimics a naturally occurring substance to stimulate a specific receptor

Question 2

Antagonist

Answer 2

Drug binds to a receptor without activating it in order to block other potential substances from activating the receptor

Question 3

Therapeutic Index

Answer 3

TD/ED (toxic dose in 50% of subjects / effective dose in 50% of subjects)

Question 4

Pharmokinetics

Answer 4

The process by which a drug is absorbed, distributed, metabolized, and eliminated by the body

Question 5

Metabolism

Answer 5

Deactivation by the liver with GI tract and other organs breaking the drug down to a less extent

Question 6

Elimination/excretion

Answer 6

Primarily by the kidneys

Question 7

Clearance

Answer 7

Volume of plasma from which a drug is eliminated per unit time

Question 8

Half-life

Answer 8

Time required to reduce the plasma drug concentration by 50%

Question 9

Decreased metabolism

Answer 9

• Decreased clearance
• Increased half life
• Increased plasma

Question 10

Increased metabolism

Answer 10

• Increased clearance
• Decreased half life
• Decreased plasma

Question 11

Mechanisms of anti-psychotics towards managing agitation

Answer 11

Inhibiting dopamine transmission

Question 12

Typical anti-psychotics

Answer 12

• Cholorpromazine
• Haloperidol
• Perphenazine
• Fluphenazine

Question 13

Second generation medications (“atypical”) treat…

Answer 13

• Depressive states

Question 14

Adverse effects of psychotics

Answer 14

• Rigidity, tremors
• TD
• OH
• Change in weight, glucose/lipid levels
• Dizziness

Question 15

Benzodiazepines (treat + mechanism)

Answer 15

• Treat anxiety, seizures, spasticity, anesthesia, sedative
• Binds to GABA receptors to cause hyper-polarization and inhibit neuronal firing
• *Can lead to physical dependence, withdrawal symptoms

Question 16

Benzodiazepines ending

Answer 16

“-AM”

• Estazolam
• Flurazepam
• Queazepma
• Clonazepam

Question 17

Non-benzo meds = Barbituates (treat + mechanism)

Answer 17

• Use to promote sleep, also a good anesthetic
• Binds to GABA receptors = cause decreased arousal and increased sleepiness
• *HIGHLY ADDICTIVE with small therapeutic index

Question 18

Barbituates ending

Answer 18

“-AL”

• Amobarbital
• Phenobarbital
• Pentobarbital

Question 19

Most commonly prescribed non-benzos

Answer 19

• Zaleplon (Sonata)
• Zolpidem (Ambien)
• Eszopiclone (Lunesta)

Question 20

Precedes (treat + mechanism)

Answer 20

• Used as a sedative in ICUs to control agitation
• Binds to alpha-2 receptor to decreased sympathetic response
• *May cause bradycardia or hypotension

Question 21

Partial seizure

Answer 21

Simple - may cause motor, sensory, autonomic,or psychological symptoms without obvious change in consciousness

• Complex - focal seizure activity with impaired consciousness
• *May spread across hemispheres and become generalized

Question 22

Generalized seizure

Answer 22

• Simple - brief loss of consciousness without any detectable signs
• Complex - loss of consciousness with notable clinical signs present
• Absence (petit mal) - brief lapses without loss of postural control
• Tonic-clinic - loss of consciousness with violent muscle contractions

Question 23

First-line medications of partial seizures

Answer 23

• Carbamzepine (Tegretol)
• Phenytoin (Dilantin)
• Oxcarbazepine (Trileptal)
• Valproic acid (Valproate)

Question 24

FIrst-line medications for generalized tonic-clinic seizures

Answer 24

• Valproic acid (Valproate)
• Lamotrigine (Lamictal)
• Topiramate (Topamax)

Question 25

Anti-seizure mechanism of action and side effects

Answer 25

``` Mechanism - blockaded of voltage gated sodium channels Common side effects - Nausea - Dizziness - Poor coordination - Drowsiness/sleepiness - Diplopia ```

Question 26

Neurostimulants mechanism

Answer 26

- Increases synaptic concentration of dopamine, serotonin, and non-adrenaline - Increases neuronal sprouting and synaptogensis - Increases synaptic efficiency by facilitating long-term potentiation

Question 27

Neurostimulant types

Answer 27

- Ritaline - Amphetamine - DA agonists

Question 28

Tizanidine (mechanism + treat)

Answer 28

- Centrally acting alpha-2 adrenergic agonists which decreases polysnynaptic reflex activity - Used in conditions of marked muscle weakness

Question 29

Tizanidine side effects

Answer 29

- Hypotension - Elevated liver enzymes - Sedation - Hallucinations

Question 30

Baclofen (mechanism + treat)

Answer 30

- Acts centrally by binding to GABA receptors and inhibits spinal reflexes - Used when muscle weakness is not severe

Question 31

Baclofen side effects

Answer 31

- Sedation - Muscle weakness - Confusion - Dyskinesia - Hallucinations

Question 32

Diazepam (Benzo) (mechanism + treat)

Answer 32

- Centrally acting by inhibiting GABA receptors and pre-synaptic/postsynaptic reflexes - Used with painful spams especially at night

Question 33

Diazepam side effects

Answer 33

- Sedation | - Habituation

Question 34

Dantrolene sodium (mechanism + treat)

Answer 34

- Acts directly on skeletal muscle by prevention release of calcium from SR - Used with severe spasms and spinal cord lesions

Question 35

Dantrolene sodium side effects

Answer 35

- Weakness - Diarrhea - Hepatotoxicity

Question 36

Clonodine (mechanism, treat, + side effects)

Answer 36

- Decreases polysynaptic reflex activity - Used with spasticity associated with uncontrolled HTN - Side effects: OH

Question 37

Gabapentin (mechanism, treat, + side effects)

Answer 37

- Similar structure to GABA, mechanism unknown - Used with MS and SCI - Side effects: sedation, confusion, fatigue, weight gain

Question 38

Botox (mechanism + lasting effects)

Answer 38

- Acts on NMJ by inhibiting release of ACH at pre-synaptic terminal - Effects last for 2-6 months