Pharm 32

Question 1

o MOA: agonize 5-HT1 receptors

○ Leads to vasoconstriction of painfully dilated meningeal, dural, cerebral, and pial vessels

○ Inhibits dural vasodilation and inflammation

○ Inhibits trigeminal nuclear excitability

Answer 1

triptan MOA

sumatriptan, frovatriptan, zolmitriptan

Question 2

triptan drugs

sumatriptan, frovatriptan, zolmitriptan

Answer 2

o Minor differences in pharmacokinetic or receptor affinity exist across these drugs, but for most patients, the agents are interchangeable
o Choice is usually dictated by cost/formulary availability

Question 3

When are triptan drugs most effective

Answer 3

○ Taken at onset of migraine
○ Combined with an NSAID
○ NOT overused
○ No opioid use recently

Question 4

Sumatriptan

Answer 4

used most often - rapid and short acting

Question 5

Frovatriptan

Answer 5

used for menstrual migraines

Question 6

Ergot alkaloids use

Answer 6

acute migraine treatment

Question 7

Potent vasoconstrictor MOA

Answer 7

ergot alkaloids

Question 8

Formulations of ergot alkaloids

Answer 8

always include caffeine to improve bioavailability

Question 9

○ DO NOT combo with other vasoconstrictors or use on anyone who cannot tolerate a vasoconstrictor
§ Such as in peripheral vascular disease
§ Individuals already on “triptans”
§ Must monitor BP and for angina/peripheral vascular ischemia
○ Cold fingers and toes!

Answer 9

Ergot alkaloids ADE

Question 10

○ Dysphoria
○ Nausea
○ Vomiting
○ Cardiovascular effects
○ Greater cost of oral formulations

Answer 10

Ergot alkaloids ADE

Question 11

Primary role of muscle relaxants in spasticity

Answer 11

pts with underlying spastic syndromes

Question 12

muscle relaxants role in musculoskeletal pain

Answer 12

Adjunct to NSAIDs, and/or opioids for MSK pain

Question 13

Peripheral GABA receptors

Answer 13

Baclofen

Question 14

Alpha 2 adrenergic agonist MOA

Answer 14

tizanidine

Question 15

GABA-A and GABA-B allosteric agonists (opens Cl- channels)

Answer 15

diazepam

Question 16

general CNS depressant

Answer 16

methocarbamol

cyclobenzaprine

Question 17

Interferes with the release of calcium ions from the sarcoplasmic reticulum

Answer 17

dantrolene

Question 18

□ Administered via intrathecal route for severe spasticity

Reduces motor neuron excitability/spasticity; relieves clonus, flexor spasms, muscle rigidity

Answer 18

baclofen

Question 19

Management of spasticity
Similar uses as baclofen
Common OFF LABEL use is for acute low back pain

Answer 19

tizanidine

Question 20

Chronic spastic syndromes (usually oral) and malignant hyperthermia (IV)

Not a regular go-to for lower spastic back pain due to HEPATOTOXICITY

Answer 20

dantrolene

Question 21

Acute, painful muscle spasms associated with musculoskeletal conditions

□ DO NOT combine with TCAs due to similar structure –> toxicity
□ STRONG anticholinergic
□ Sedation

Answer 21

cyclobenzaprine

Question 22

Adjunctive treatment of muscle spams associated with acute painful musculoskeletal conditions

Answer 22

methocarbamol

Question 23

§ Use: Muscle spasms, Spasticity

§ ADE: Tolerance, dependence, CNS depression, abuse

§ PKs: Unpredictable and undergo a variable duration of action; Accumulates in tissues

Answer 23

diazepam

Question 24

Schedule 4 drug

§ ADE
□ Tolerance, dependence, CNS depression, abuse
□ MAX recommendation in therapy length: 2-3 weeks
□ Longer treatments are associated with withdrawal

Answer 24

carisoprodol

Question 25

Activates peripheral nociceptors on primary sensory neurons to temporary increase release of substance P Eventually leads to depletion of substance P in neurons to relieve neuronal firing

Answer 25

capsaicin

Question 26

good for insect bites, minor burns/cuts/scrapes, poison oak/ivy/sumac, eczema, psoriasis, dry skin

Answer 26

menthol

Question 27

Methyl salicylate

Answer 27

§ Combined with trolamine salicylate to form "Aspercreme" □ Intraarticular salicylic acid concentrations can reach 60% of those provided by large systemic doses of ASA --> CHEAP □ Useful for mild musculoskeletal and arthritic pain

Question 28

NSAID that is topical and transdermal

Answer 28

diclofenac

Question 29

§ VERY low doses of an NSAID, but still warned about the systemic effects of taking an NSAID □ CV thrombotic events, GI effects (ulcers, bleeding, perfs), renal, HTN, CHF, pregnancy, liver warnings □ PREGNANCY: may cause premature closure of ductus arteriosus

Answer 29

diclofenac

Question 30

ASA triad

Answer 30

chronic rhinosinusitis, nasal polyps, severe bronchial asthma

Question 31

local anesthetics MOA

Answer 31

blocks sodium channels to prevent the pain signal impulse from conducting along the afferent nerve Suppresses the perception of the pain occurring

Question 32

○ Why the anesthesia may fail | § Pharmacokinetic reasons

Answer 32

□ Increased local blood flow/distribution away from site of injection □ Local tissue acidosis/edema - like during infections □ Patients with higher rates of metabolism

Question 33

○ Why the anesthesia may fail | § Pharmacodynamic reasons

Answer 33

□ Effects of inflammation on peripheral and central sensitization of nerves □ Patients with less susceptible nerve fibers

Question 34

ADE: cardiac of local anesthetics

Answer 34

□ AV block □ Dysrhythmias □ Bradycardia/Hypotension □ Cardiac arrest

Question 35

ADE: neurological of local anesthetics

Answer 35

□ CNS excitation followed by depression □ Spinal HA □ Autonomic blockades results in urinary/fecal incontinence

Question 36

Lidocaine vs. ropivacaine

Answer 36

lidocaine: faster acting ropivacaine: longer acting with half life >4hrs

Question 37

benzocaine vs. tetracaine

Answer 37

benzocaine more prone to methemoglobinemia

Question 38

Any history of CV disease, heart disease, or hepatic impairment, contraindicates this use

Answer 38

ergotamine/dihydroergotamine

Question 39

Why is caffeine in ergotamine for migraine treatment?

Answer 39

Caffeine increases the bioavailability of ergotamines Caffeine can help with the migraine

Question 40

Factors that increase triptan effectiveness to treat migraine

Answer 40

a. Taken at very onset of migraine b. Combined with an NSAID c. Not overused d. Opioid use not recent

Question 41

Factors that decrease triptan effectiveness to treat migraine

Answer 41

a. Waiting to take the med b. Not combined with an NSAID c. Used frequently already d. Have a contraindication

Question 42

Rapid-acting, and therefore potentially more effective as migraine and cluster headache abortive therapies

Answer 42

sumatriptan

Question 43

Longer-acting, and therefore potentially more useful for menstrual or other similarly timed recurring migraines

Answer 43

frovatriptan

Question 44

Describe and compare contraindications of the ergot alkaloids and -triptans

Answer 44

A. Cardiovascular, coronary heart disease B. HTN, uncontrolled C. Hepatic impairment (as are liver metabolized!) D. Peripheral vascular disease - ANY HISTORY, symptoms, or signs E. Hypersensitivity to drug or components

Question 45

ergotism from moderate ingestion

Answer 45

n/v

Question 46

ergotism from higher ingestion levels

Answer 46

i. Distal vasoconstriction - check for peripheral vascular ischemia! (cold fingers and toes) ii. Itching/burning limb pain iii. Loss of limb sensation iv. Gangrene/auto-amputation of charcoal-black limbs

Question 47

ergotism from convulsive levels

Answer 47

i. Flexion of fingers/wrists/ankles ii. Double vision iii. Altered mental state/mania iv. Hallucinations and diaphoresis

Question 48

OTC analgesics for tension HA tx

Answer 48

i. 1,000mg acetaminophen | ii. Ibuprofen, ASA, naproxen

Question 49

prevention of tension HA

Answer 49

i. can include amitriptyline, PT ii. PT will strengthen muscle/reduce tension, address postural deficits iii. Trigger management

Question 50

prevention of cluster HA | first choice

Answer 50

i. Verapamil is first choice for prevention 1) Does not readily cross the BBB so much have larger doses a) Do have to watch for BP dropping, swelling/edema

Question 51

prevention of cluster HA | second choice

Answer 51

ii. Lithium is first or second choice

Question 52

prevention of cluster HA | other choice

Answer 52

iii. Others: | 1) Glucocorticoids, Warfarin, Melatonin

Question 53

treatment of cluster HA

Answer 53

i. "Triptan" - rapid onset formulation --> sumatriptan | ii. Oxygen: 7 - 12 L/min by a non-rebreather mask

Question 54

reduced HA incidence

Answer 54

HTN meds

Question 55

Sources of pain relieved by Tylenol

Answer 55

a. Frequent episodic tension type HA (1,000mg) and other general Has b. Osteoarthritis pain i. NSAIDs are recommended as initial therapy for OA 1) Oral NSAIDs for hand, knee, hip OA 2) Topical NSAIDs for hand and knee OA and >75yrs

Question 56

Source of pain NOT relieved by Tylenol

Answer 56

low back pain

Question 57

A. Acute pain treatment for muscle relaxants

Answer 57

a. Methocarbamol b. Diazepam - risk for tolerance, abuse, and dependence c. Carisoprodol - risk for tolerance, abuse, and dependence d. Tizanidine - off label e. Diclofenac 1% gel for acute pain of strains, sprains, and contusions of 2-4 grams to skin of the affected areas

Question 58

B. Chronic pain treatment for muscle relaxants

Answer 58

a. Baclofen | b. Dantrolene - watch hepatotoxicity

Question 59

Capsaicin use

Answer 59

i. Post herpetic neuralgia | ii. Minor aches/pains of muscles/joints - arthritis, backache, sprains

Question 60

menthol use

Answer 60

sore throats | MSK aches/pains

Question 61

methyl salicylate use

Answer 61

arthritis | mild MSK pain

Question 62

diclofenac use

Answer 62

upper/lower extremity joint arthritis acute pain of strains/sprains/contusions

Question 63

capsaicin SE

Answer 63

i. Dose must be titrated up and can produce a burning sensation for the first few days of application ii. Lower doses produce less burning

Question 64

diclofenac SE

Answer 64

i. All indications with NSAIDs 1) CV thrombotic events, CHF, renal, liver toxicities, GI effects (ulcers, perforations, bleeds), pregnancy (premature closure of ductus arteriosus) 2) Increased sun sensitivity

Question 65

MOA of local anesthetics

Answer 65

Suppress pain by blocking the sodium channels on afferent nerves to suppress pain impulse conduction signals at the administration site to reduce the body's awareness of the pain

Question 66

local anesthetics clinical use

Answer 66

Suppresses pain without generalized depression of nervous system at correct doses and route/site of administration

Question 67

Chronological onset of local anesthetic action (5 steps to know)

Answer 67

1. anesthetic is injected near a nerve 2. local anesthetic permeates axonal neuronal membranes 3. binding of local anesthetic to sites on voltage-gated sodium channels 4. period of time when only a few sodium channels are blocked -> results are insufficient for full anesthesia 5. clinically observed rates of onset and recovery from blockade due to relatively slow diffusion of local anesthetic molecules into and out of the whole nerve.

Question 68

ester-type anesthetics (4)

Answer 68

cocaine procaine tetracaine benzocaine

Question 69

amide-type anesthetics (5)

Answer 69

``` lidocaine mepivaciane articaine bupivacaine ropivacaine ```

Question 70

Ester-type anesthetics metabolism

Answer 70

Very short plasma half-life: Therefore only administered locally and are broken down quite quickly 1/2 life renders them ineffective for systemic / significant tissue distribution

Question 71

Amide-type anesthetics metabolism

Answer 71

b. Has a much larger tissue distribution and can therefore be administered over a greater area c. Metabolized by the liver d. Great choice for wanting a longer duration of anesthetic

Question 72

cross allergenic potential with ester and amide anesthetics

Answer 72

a. If allergic to a specific ester, cannot use other ester anesthetics i. CAN use an amide-type however ii. And vice-versa b. Esters are metabolized to PABA and some individuals have a reaction to this

Question 73

adverse effects of local anesthetics that are an extension of the MOA

Answer 73

a. Difficult to control toxicity of agents due to sodium channels being required for normal function of neurons i. Blockage can result in… 1) Cardiac effects: potentially dysrhythmias 2) Central nervous system adverse effects 3) Induce seizures 4) Systemic effects when absorbed systemically/administered into highly perfused tissues

Question 74

use of epi in local anesthetics

Answer 74

- a vasoconstrictor that helps to reduce the systemic effects and prolong the local effects - helps with bleeding at the site - decreases rate of vascular absorption - increases anesthetic molecules at targeted nerve membrane - deeper and longer duration of anesthesia achieved - provides a marker for inadvertently entering a vascular vessel due to CV excitability - May have ability to activate endogenous analgesic mechanisms and produce a deeper state of anesthesia through activation and binding of alpha2 adrenergic receptors (Absorption of a vasoconstrictor itself can cause palpitations, tachycardia, nervousness, HTN)