analgesics naplex pg 132. treatment algorithm for pain patient in pain rating scale 0-10 mild pain...
TRANSCRIPT
AnalgesicsAnalgesics
NAPLEX
PG 132
Treatment Algorithm for PainTreatment Algorithm for Pain
Patient in painRating Scale 0-10
Mild Pain (0-3)NSAID, aspirin,
APAP
Moderate Pain (4-6)Weak opioid:
codeine, hydrocodone
Severe Pain (7-10)Strong opioid:
morphine, oxycodone,
hydromorphone
Treating Specific Types of Cancer Pain
Treating Specific Types of Cancer Pain
Bone pain NSAIDs, bisphosphonates, corticosteroids, opiates
Visceral pain NSAIDs, opiates
Neuropathic pain TCAs, gabapentin, carbamazepine, corticosteroids
Muscle spasms Benzodiazepines, baclofen
Bone pain NSAIDs, bisphosphonates, corticosteroids, opiates
Visceral pain NSAIDs, opiates
Neuropathic pain TCAs, gabapentin, carbamazepine, corticosteroids
Muscle spasms Benzodiazepines, baclofen
Non Opioid AnalgesicsNon Opioid Analgesics
Drug Dose Interval Renal Adjustment Hepatic Adjustment
Acetaminophen 500-1000 mg
Max: 4 g
4-6 hours GFR: >50 ml/min q4h,
10-50 ml/min q6h,
<10 ml/min q8h
1/2 life is increased,
Can be given safely
Aspirin 500- 1000 mg
Max: 4 g
4-6 hours Avoid Avoid
Celecoxib 100-200 mg
Max: 800 mg
12 hours Avoid Decrease dose by 50 %
Rofecoxib
(off market)
12.5 mg-25 mg
Max: 50 mg
Daily Avoid Avoid
Valdecoxib
(off market)
10-20 mg
Max: 40 mg
Daily Avoid Avoid
PG 134
Non Opioid Analgesics con’tNon Opioid Analgesics con’t
Drug Dose Interval Renal Adjustment Hepatic Adjustment
Ibuprofen 200-800 mg
Max: 3.2 g/day
4-6 hours Use with caution Contraindicated in renal failure
No dose alterations,
Kinetics minimally effected
Naproxen 550 mg initial,
250 subsequent
Max: 1.5g/day
6-8 hours Use with caution Reduce dose 50%
Indomethacin 25 mg
Max: 200mg/day
8-12 hours Use with caution Avoid
Ketoralac 30 mg or 60 mg IM
Max: 5 days of combine treatment (IM & PO)
6 hours Avoid Avoid
Oxicams
Carboxylic Acids
Fenamates
NaphthylalkanoneAcetic Acids
oxaprozinnaproxenibuprofenketoprofenfenoprofenflurbiprofen
Propionic Acids
meclofenamatemefenamic acid
piroxicammeloxicam
sulindacetodolacindomethacintolmetindiclofenacketorolac
nabumetone
GI Sparing Agents
diclofenac/misoprostoldiclofenac/misoprostol
Salicylates
ASA
NonacetylatedSalicylates
salsalatediflunisalcholine
Weak Opioid AnalgesicsWeak Opioid AnalgesicsDrug Dose Interval Renal Adjustment Hepatic Adjustment
Codeine 15-60 mg
Max: 120 mg
4-6 hours CrCl:
10-50 ml/min=75% of dose,
<10 ml/min=50% of dose
A dosage adjustment decrease
Oxycodone w/
-acetaminophen
-aspirin
5 mg
Max: 4 g* 4-6 hours
Be conservative, drug levels increase by 50%
1/3 to 1/2 of usual dose,
Elimination 1/2 life increase by 2.3 hours
Hydrocodone w/
-ibuprofen (7.5/200)
-acetaminophen
(5/500)
-aspirin
(5/500)
1-2 tabs
Max: 5 tabs
1-2 tabs
Max: 4 g*
1-2 tabs
Max: 4 g*
4-6 hours
4-6 hours
4-6 hours
Use cautiously in mild to moderate renal failure, avoid in severe renal failure
Avoid
Tramadol
-acetaminophen
(37.5/325)
50-100 mg
Max: 400mg
2 tabs
Max: 8 tabs
4-6 hours
4-6 hours
CrCl < 30 ml/min increase dosing interval to q12h with a max of 200 mg per day
Cirrhosis 50 mg q12h
Avoid
Weak Opioid Analgesics con’tWeak Opioid Analgesics con’tDrug Dose Interval Renal Adjustment Hepatic Adjustment
Propoxyphene
-acetaminophen
-aspirin
1-2 tabs
Max: 4 g*
1-2 tabs
4 hours
4 hours
Don’t give in severe renal failure, use cautiously in mild and moderate renal failure
Avoid
Strong Opioid AnalgesicsStrong Opioid AnalgesicsDrug Dose Interval Renal Adjustment Hepatic
Adjustment
Meperidine
- Binds opiate receptors
50 - 150 mgMetabolite accumulation (normeperidine) Anxiety, agitation, tremor &/or seizures
3-4 hours GFR
>50 ml/min No adjustment
10-50 ml/min 75% of dose
<10 ml/min 50% of dose
Decrease dose, 1/2 life is increased
Morphine (gold standard)
-immediate release
-IV, IM, SQ,
continuous infusion
-epidural
-intrathecal
-rectal
10-30 mg
2.5-20 mg
0.8 to 10 mg/hr
Max: 80 mg/hr
5mg bolus, redose 1 hr 1 to 2 mg
Max: 10 mg/24 hr
0.2 to 1 mg
10-20 mg
Titrate to response
2-6 hours
No repeat dose
4 hours
GFR
>50 ml/min No adjustment
10-50 ml/min 75% of dose
<10 ml/min 50% of dose
(morphine-6-glucuronide) accumulates in renal failure
1/2 life prolonged increase interval by 1.5 to 2 times
Strong Opioid Analgesics con’tStrong Opioid Analgesics con’tDrug Dose Interval Renal Adjustment Hepatic Adjustment
Hydromorphone
-PO, IM, IV, SQ
-rectal
1-4 mg
3 mg
4-6 hours
6-8 hours
Decrease dose
Oxycodone
- percocet (APAP)
- percodan (ASA)
5 mg
May titrate to response – no maximum dose
6 hours – Be conservative, drug levels increase by 50%
1/3 to 1/2 of usual dose,
Elimination 1/2 life increase by 2.3 hours
Methadone
-PO, IM, SQ
-IV
2.5-10 mg
Max:1000 mg
0.1mg/kg
3-8 hours
4 hrs x 3 doses then 6-12 hours
GFR
>50ml/min q6h
10-50 ml/min q8h
<10 ml/min q12h
CrCl
<10 ml/min 50-75% dose
No Change in dose mild to moderate disease,
Avoid in severe liver disease
Strong Opioid Analgesics con’tStrong Opioid Analgesics con’tDrug Dose Interval Renal Adjustment Hepatic Adjustment
Fentanyl
-transdermal
-transmucosal-Parenteral
Initial 25 mcg/hr
Initial 200 mcg
72 hours
30 min
CrCl
10-50 ml/min 75% of dose
<10 ml/min 50% of dose
Unaffected by cirrhosis, effected by hepatic blood flow
Remind patients that heat can increase fentanyl absorption. Remind patients that heat can increase fentanyl absorption. Warn against extended exposure of the patch to heating pads, Warn against extended exposure of the patch to heating pads, hot tubs, sunbathing, high fever, etc.hot tubs, sunbathing, high fever, etc.
Opioid Equianalgesic DosingOpioid Equianalgesic DosingDrug Oral (mg) Parenteral (mg)
Morphine 30 10
Hydromorphone 7.5 1.5
Oxycodone 20-30 10-15
Methadone 10-20 acute?
2-4 chronic
10 acute?
2-4 chronic
Levorphanol 4 acute
1 chronic
2 acute
1 chronic
Fentanyl x 0.1-0.2
Oxymorphone x 1
Meperidine 300 75
Morphine Analogs---table 2-28, pg.132
General propertiesGeneral properties
CNS depressionCNS depression
Respiratory depressionRespiratory depression
Reduce propulsive activity of the gut Reduce propulsive activity of the gut
Urinary retentionUrinary retention
Toxicity causes pinpoint pupilsToxicity causes pinpoint pupils
No maximum doseNo maximum dose
Meperidine Analogs---See Table 2-28, pg.132Meperidine Analogs---See Table 2-28, pg.132
General properties
Good analgesic (parenteral)
Less CNS depression or constipation than opiates
Spasmolytic action - may be useful for pain related to uterus, GI, bronchi, etc.
Combination with hydroxyzine or promethazine permits 25–50% dosage reduction
Principal drugs
Meperidine (Demerol)---accumulates in renal disease, metabolite can cause siezures
Diphenoxylate + atropine (Lomotil) – C-V
- antidiarrhea- subtherapeutic dose of atropine to prevent abuse
PG 133
Drugs for MigraineDrugs for Migraine
Headache TypesHeadache Types
- - Tension, Cluster, MigraineTension, Cluster, Migraine
- Migraine is unilateral, pulsating, throbbing, with - Migraine is unilateral, pulsating, throbbing, with or w/o aura, or w/o aura,
nausea, photophobia, sonophobia nausea, photophobia, sonophobia
TreatmentsTreatments – – Prophylactic and AbortiveProphylactic and Abortive
AbortiveAbortiveAspirin - analgesic, antipyretic, anti-inflammatory, anti-plateletAspirin - analgesic, antipyretic, anti-inflammatory, anti-platelet
Acetaminophen—analgesic, antipyreticAcetaminophen—analgesic, antipyretic
NSAIDs - analgesic, antipyretic, anti-inflammatory (See Table pg. NSAIDs - analgesic, antipyretic, anti-inflammatory (See Table pg. 133)133)
• • Mechanism of actionMechanism of action
• • Common adverse effects: GI toxicity, hypersensitivity, renal effectsCommon adverse effects: GI toxicity, hypersensitivity, renal effects
Contraindications to the use of Imitrex include which of the following:
I. uncontrolled HTNII. use of and MAOI within the past 2
weeksIII. ischemic heart disease
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Contraindications to the use of Imitrex include which of the following:
I. uncontrolled HTNII. use of and MAOI within the past 2
weeksIII. ischemic heart disease
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Contraindications to the use of Imitrex include which of the following:
I. uncontrolled HTNII. use of and MAOI within the past 2
weeksIII. ischemic heart disease
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Contraindications to the use of Imitrex include which of the following:
I. uncontrolled HTNII. use of and MAOI within the past 2
weeksIII. ischemic heart disease
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
PG 132
Drugs for Migraine
Abortive - (cont.)Abortive - (cont.)Dihydroergotamine (Migranal)Dihydroergotamine (Migranal)nasal spray; dose may be repeated nasal spray; dose may be repeated after 15 min – after 15 min – MOA – blocks alpha adrenergic causing vasoconstritionMOA – blocks alpha adrenergic causing vasoconstrition
5-HT15-HT1DD Receptor Agonists Receptor Agonistsavoid in patients with cardiovascular avoid in patients with cardiovascular diseasedisease
• • Almotriptan (Axert)Almotriptan (Axert)
• • Eletriptan (Relpax) – tablets; newest agent on the market – another “me-too”Eletriptan (Relpax) – tablets; newest agent on the market – another “me-too”
• Frovatriptan (Frova) – tablets; longest half life among agents
• • Naratriptan (Amerge) - tablets Naratriptan (Amerge) - tablets
• • Rizatriptan (Maxalt) - tablets; also Maxalt MLT Rizatriptan (Maxalt) - tablets; also Maxalt MLT (oral disintegrating tab)(oral disintegrating tab)
•• Sumatriptan (Imitrex) - Sumatriptan (Imitrex) - injection, tablet, nasal sprayinjection, tablet, nasal spray
• • Zolmitriptan (Zomig) - tablets; also Zomig ZMT (oral disintegrating tab)Zolmitriptan (Zomig) - tablets; also Zomig ZMT (oral disintegrating tab)
PG 133
Drugs for Migraine
Prophylactic Therapy
- Given to patients with >2-3 HA/month, severe HA, ineffective
treatment
Drugs of Choice:
- propranolol (Inderal) – use if patient also has HTN
- amitriptyline (Elavil) – concomitant depression
- valproate (Depakote) - concomitant seizures
Other agents:
- verapamil, topiramate
PathophysiologyPathophysiology
ComplicationsComplications
Source: www.arava.com
Rheumatoid ArthritisRheumatoid Arthritis Corticosteroids – early, acute, not long-term
- also NSAIDs / COX-2 Inhibitors
Disease Modifying Antirheumatic Drugs (DMARDs) – Disease Modifying Antirheumatic Drugs (DMARDs) – liver, hemeliver, hemeAuranofin (Ridaura) Auranofin (Ridaura) Aurothioglucose (Solganol)Aurothioglucose (Solganol)Azathioprine (Imuran)Azathioprine (Imuran)Cyclophosphamide (Cytoxan) Cyclophosphamide (Cytoxan) Cyclosporine (Neoral, Sandimmune) Cyclosporine (Neoral, Sandimmune) Gold sodium thiomalate (Myochrysine) Gold sodium thiomalate (Myochrysine) Hydroxychloroquine (Plaquenil)Hydroxychloroquine (Plaquenil) – retinal toxicity – Q 6 months – retinal toxicity – Q 6 monthsMethotrexate (Rheumatrex)Methotrexate (Rheumatrex)Leflunomide (Arava)---Preg Cat X, long half-life, hepatotoxicLeflunomide (Arava)---Preg Cat X, long half-life, hepatotoxic Penicillamine (Cuprimine, Depen)Penicillamine (Cuprimine, Depen)Sulfasalazine (Azulfindine) – orange-yellow urineSulfasalazine (Azulfindine) – orange-yellow urine
Corticosteroids – early, acute, not long-term - also NSAIDs / COX-2 Inhibitors
Disease Modifying Antirheumatic Drugs (DMARDs) – Disease Modifying Antirheumatic Drugs (DMARDs) – liver, hemeliver, heme
Auranofin (Ridaura) Auranofin (Ridaura) Aurothioglucose (Solganol)Aurothioglucose (Solganol)Azathioprine (Imuran)Azathioprine (Imuran)Cyclophosphamide (Cytoxan) Cyclophosphamide (Cytoxan) Cyclosporine (Neoral, Sandimmune) Cyclosporine (Neoral, Sandimmune) Gold sodium thiomalate (Myochrysine) Gold sodium thiomalate (Myochrysine) Hydroxychloroquine (Plaquenil)Hydroxychloroquine (Plaquenil) – retinal toxicity – Q 6 months – retinal toxicity – Q 6 monthsMethotrexate (Rheumatrex)Methotrexate (Rheumatrex)Leflunomide (Arava)---Preg Cat X, long half-life, hepatotoxicLeflunomide (Arava)---Preg Cat X, long half-life, hepatotoxic Penicillamine (Cuprimine, Depen)Penicillamine (Cuprimine, Depen)Sulfasalazine (Azulfindine) – orange-yellow urineSulfasalazine (Azulfindine) – orange-yellow urine
PG 134
GoldGold
Biologic Response ModifiersBiologic Response Modifiers
Etanercept (Enbrel) – avoid with live vaccine Etanercept (Enbrel) – avoid with live vaccine (soluble receptor TNF (soluble receptor TNF inhibitor)inhibitor)Anakinra (Kineret) – monitor for pulmonary problems Anakinra (Kineret) – monitor for pulmonary problems (IL-1 receptor (IL-1 receptor antagonist)antagonist)Infliximab (Remicade) – monitor for infection Infliximab (Remicade) – monitor for infection (monoclonal antibody (monoclonal antibody for TNF)for TNF)Adalimumab (Humira) – monitor for infection Adalimumab (Humira) – monitor for infection (monoclonal antibody (monoclonal antibody for TNF receptor)for TNF receptor)
Abatacept (Orencia®) – monitor for infection (Inhibits T-Cell (T-lymphocytes activation by binding to CD80 and CD86 on antigen presenting cells)
Osteoarthritis (OA)Osteoarthritis (OA)- acetaminophen & NSAIDs- acetaminophen & NSAIDs- surgery – knee/hip replacement- surgery – knee/hip replacement- glucosamine/chondrotin – NIH study (GAIT)- glucosamine/chondrotin – NIH study (GAIT)
Biologic Response ModifiersBiologic Response Modifiers
Etanercept (Enbrel) – avoid with live vaccine Etanercept (Enbrel) – avoid with live vaccine (soluble receptor TNF (soluble receptor TNF inhibitor)inhibitor)Anakinra (Kineret) – monitor for pulmonary problems Anakinra (Kineret) – monitor for pulmonary problems (IL-1 receptor (IL-1 receptor antagonist)antagonist)Infliximab (Remicade) – monitor for infection Infliximab (Remicade) – monitor for infection (monoclonal antibody (monoclonal antibody for TNF)for TNF)Adalimumab (Humira) – monitor for infection Adalimumab (Humira) – monitor for infection (monoclonal antibody (monoclonal antibody for TNF receptor)for TNF receptor)
Abatacept (Orencia®) – monitor for infection (Inhibits T-Cell (T-lymphocytes activation by binding to CD80 and CD86 on antigen presenting cells)
Osteoarthritis (OA)Osteoarthritis (OA)- acetaminophen & NSAIDs- acetaminophen & NSAIDs- surgery – knee/hip replacement- surgery – knee/hip replacement- glucosamine/chondrotin – NIH study (GAIT)- glucosamine/chondrotin – NIH study (GAIT)
PG 134
Joint Distribution: RA Compared to OARheumatoid Arthritis Osteoarthritis
SLE (systemic lupus erythematosus) occurs more frequently in:
a. male African Americans
b. Asians
c. post-menopausal women
d. people of Mediterranean origin
e. young women
SLE (systemic lupus erythematosus) occurs more frequently in:
a. male African Americans
b. Asians
c. post-menopausal women
d. people of Mediterranean origin
e. young women
SLE (systemic lupus erythematosus) occurs more frequently in:
a. male African Americans
b. Asians
c. post-menopausal women
d. people of Mediterranean origin
e. young women
SLE (systemic lupus erythematosus) occurs more frequently in:
a. male African Americans
b. Asians
c. post-menopausal women
d. people of Mediterranean origin
e. young women
Patients who are life time smokers have the greatest risk of leg pain associated with? a. hypokalemia
b. rhabdomylosisc. intermittent claudicationd. dopamine deficiency e. myocardial infarction
Patients who are life time smokers have the greatest risk of leg pain associated with? a. hypokalemia
b. rhabdomylosisc. intermittent claudicationd. dopamine deficiency e. myocardial infarction
Patients who are life time smokers have the greatest risk of leg pain associated with? a. hypokalemia (cramps)
b. rhabdomylosis (statins)c. intermittent claudication (PVD)d. dopamine deficiency (RLS)e. myocardial infarction
Patients who are life time smokers have the greatest risk of leg pain associated with? a. hypokalemia (cramps)
b. rhabdomylosis (statins)c. intermittent claudication (PVD)d. dopamine deficiency (RLS)e. myocardial infarction
Trigeminal neuralgia is treated by the use of:
a. aspirin
b. carbamazepine
c. dipyridamole
d. methylprednisolone
e. thiamine
Trigeminal neuralgia is treated by the use of:
a. aspirin
b. carbamazepine
c. dipyridamole
d. methylprednisolone
e. thiamine
Trigeminal neuralgia is treated by the use of:
a. aspirin
b. carbamazepine
c. dipyridamole
d. methylprednisolone
e. thiamine
Trigeminal neuralgia is treated by the use of:
a. aspirin
b. carbamazepine
c. dipyridamole
d. methylprednisolone
e. thiamine
When dispensing a prescription for Robitussin AC, the pharmacist should attach label(s) indicating:
I. May cause drowsinessII. Shake well before usingIII. Finish all of this medication
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
When dispensing a prescription for Robitussin AC, the pharmacist should attach label(s) indicating:
I. May cause drowsinessII. Shake well before usingIII. Finish all of this medication
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
When dispensing a prescription for Robitussin AC, the pharmacist should attach label(s) indicating:
I. May cause drowsinessII. Shake well before usingIII. Finish all of this medication
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
When dispensing a prescription for Robitussin AC, the pharmacist should attach label(s) indicating:
I. May cause drowsinessII. Shake well before usingIII. Finish all of this medication
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Which of the following is/are appropriate warning(s) for the use of Duragesic transdermal system patches?
I. Do not cut patches before applyingII. Not intended for use in children under
the age of 12III. Replace patch every day unless pain is
under control a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Which of the following is/are appropriate warning(s) for the use of Duragesic transdermal system patches?
I. Do not cut patches before applyingII. Not intended for use in children under
the age of 12III. Replace patch every day unless pain is
under control a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Which of the following is/are appropriate warning(s) for the use of Duragesic transdermal system patches?
I. Do not cut patches before applyingII. Not intended for use in children under
the age of 12III. Replace patch every day unless pain is
under control a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Which of the following is/are appropriate warning(s) for the use of Duragesic transdermal system patches?
I. Do not cut patches before applyingII. Not intended for use in children under
the age of 12III. Replace patch every day unless pain is
under control a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
The upper daily dosing regimen for naproxen is NOT more than:
a. 0.5 g
b. 1 g
c. 1.5 g
d. 2.5 g
e. 4 g
The upper daily dosing regimen for naproxen is NOT more than:
a. 0.5 g
b. 1 g
c. 1.5 g
d. 2.5 g
e. 4 g
The upper daily dosing regimen for naproxen is NOT more than:
a. 0.5 g
b. 1 g (mefenamic)
c. 1.5 g (naproxen)
d. 2.5 g
e. 4 g (acetaminophen)
Ibuprofen (3.2g) Indomethacin (200mg)
The upper daily dosing regimen for naproxen is NOT more than:
a. 0.5 g
b. 1 g (mefenamic)
c. 1.5 g (naproxen)
d. 2.5 g
e. 4 g (acetaminophen)
Ibuprofen (3.2g) Indomethacin (200mg)
Which of the following ingredients is are present in Percodan but not in Percocet:
I. AspirinII. AcetaminophenIII. Oxycodone
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Which of the following ingredients is are present in Percodan but not in Percocet:
I. AspirinII. AcetaminophenIII. Oxycodone
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Which of the following ingredients is are present in Percodan but not in Percocet:
I. AspirinII. AcetaminophenIII. Oxycodone
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Which of the following ingredients is are present in Percodan but not in Percocet:
I. AspirinII. AcetaminophenIII. Oxycodone
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Drugs for the Treatment of Asthma
Drugs for the Treatment of Asthma
NAPLEX
PG 142
Symptoms Nighttime Symptoms
Lung Function
Step 1Mild
Intermittent
Symptoms ≤ 2 times a week Asymptomatic and normal PEF between exacerbations Exacerbations brief (from a few hours to a few days); intensity may vary
≤ 2 times a month FEV1/PEF ≥ 80% predicated PEF variability < 20%
Step 2Mild
Persistent
Symptoms > 2 times a week but < 1 time a day Exacerbations may affect activity
> 2 times a month FEV1/PEF ≥ 80% predicated PEF variability < 20-30%
Step 3ModeratePersistent
Daily symptoms Daily use of inhaled short-acting beta-2 agonist Exacerbations affect activity Exacerbations ≥ 2 times a week; may last day
> 1 time a week FEV1/PEF > 60 - < 80% predicated PEF variability > 30%
Step 4Severe
Persistent
Continual Symptoms Limited Physical Activity Frequent Exacerbations
Frequent FEV1/PEF ≤ 60% predicated PEF variability > 30%
Classification
PG 142
Drugs for the Treatment of AsthmaDrugs for the Treatment of Asthma
phosphodiesterasephosphodiesterase
Adenyl cyclaseAdenyl cyclase cyclic AMP (bronchodilation) cyclic AMP (bronchodilation) eliminationelimination
SympathomimeticsSympathomimetics
Increase formation of cyclic AMPIncrease formation of cyclic AMP
NonselectiveNonselective
• • EphedrineEphedrine
• • Epinephrine (Adrenalin, Medihaler-Epi, Bronkaid, Primatene, Epinephrine (Adrenalin, Medihaler-Epi, Bronkaid, Primatene, etc.)etc.)
• • Ethylnorepinephrine (Bronkephrine)Ethylnorepinephrine (Bronkephrine)
PG 143
Drugs for the Treatment of AsthmaDrugs for the Treatment of Asthma
Selective Short-Acting Beta-2 Agonists. Selective Short-Acting Beta-2 Agonists. Provide Provide quick relief; may cause tachycardia, tremor, etc.quick relief; may cause tachycardia, tremor, etc.
• • Albuterol (Proventil, Ventolin, Airet, Albuterol (Proventil, Ventolin, Airet, Volmax) Volmax) 0.5hr peak, 4 0.5hr peak, 4 hours durationhours duration
• • Albuterol - oral sustained-release productAlbuterol - oral sustained-release product
• • Pirbuterol (Maxair) – Pirbuterol (Maxair) – Autoinhaler – longer duration 6 Autoinhaler – longer duration 6 hrs (tertiary butyl hrs (tertiary butyl group) group)
• • Levalbuterol (Xopenex) – Levalbuterol (Xopenex) – active isomer of albuterol, active isomer of albuterol, neb., less cardiac neb., less cardiac side effects side effects
• • Metaproterenol (Alupent, Metaprel) – Metaproterenol (Alupent, Metaprel) – delayed delayed onset (1 hour) & onset (1 hour) & prolonged prolonged effect (4 hour)effect (4 hour)
• • Terbutaline (Brethine, Bricanyl) – Terbutaline (Brethine, Bricanyl) – delayed onset delayed onset 1 hour & prolonged duration (6hr) – no-inhalation in U.S. & (management 1 hour & prolonged duration (6hr) – no-inhalation in U.S. & (management of pretermed labor)of pretermed labor)
• • isoproterenol (Isuprel, Medihaler-Iso) – isoproterenol (Isuprel, Medihaler-Iso) – beta-1 & beta-2 activitybeta-1 & beta-2 activity
Drugs for the Treatment of Asthma (cont.)
Long-Acting Beta-2 Agonists. Long-Acting Beta-2 Agonists. For long-term symptom control; For long-term symptom control; frequently used with frequently used with inhalational corticosteroids; may cause inhalational corticosteroids; may cause tachycardia, tremor,tachycardia, tremor, etc.; for prophylaxis only. etc.; for prophylaxis only.
• • Formoterol (Foradil) – DPI - capsuleFormoterol (Foradil) – DPI - capsule
• • Salmeterol (Serevent) – DPI – DiskusSalmeterol (Serevent) – DPI – Diskus
NOT SUITABLE AS A RESCUE INHALER!!!!!!!!!!!!!!NOT SUITABLE AS A RESCUE INHALER!!!!!!!!!!!!!!
PG 142
PG 142
Drugs for the Treatment of Asthma
XanthinesXanthinesPhosphodiesterase inhibitors; generally for prophylaxis; adverse Phosphodiesterase inhibitors; generally for prophylaxis; adverse effects similar to caffeineeffects similar to caffeine
• • Theophylline (Slo-Phyllin, Theolair, Theo-Dur)----Think Theophylline (Slo-Phyllin, Theolair, Theo-Dur)----Think drug interactions, serum levels 10-20, arryhthimogenic at high drug interactions, serum levels 10-20, arryhthimogenic at high levelslevels
• • Dyphylline (Lufyllin)Dyphylline (Lufyllin)theophylline derivativetheophylline derivative
• • Aminophylline (Somophyllin-CRT)Aminophylline (Somophyllin-CRT)anhydrous contains anhydrous contains 86% 86%
- 300mg theo (PO) = 380mg Amino (IV)- 300mg theo (PO) = 380mg Amino (IV)
theophylline, dihydrate 79%theophylline, dihydrate 79%
• • Oxtriphylline (Choledyl)Oxtriphylline (Choledyl)contains 64% theophyllinecontains 64% theophylline
Leukotriene receptor drugsLeukotriene receptor drugsFor prophylaxis; may reduce need for beta-2 agonistFor prophylaxis; may reduce need for beta-2 agonist
• • Zafirlukast (Accolate)Zafirlukast (Accolate)leukotriene receptor antagonistleukotriene receptor antagonist
• • Montelukast Sodium (Singulair)Montelukast Sodium (Singulair) leukotriene receptor leukotriene receptor antagonistantagonist
• • Zileuton (Zyflo)Zileuton (Zyflo)inhibits leukotriene formation (5-inhibits leukotriene formation (5-lipoxygenase inhibitor); lipoxygenase inhibitor);
monitor hepatic function, think DIs---potent inhibitormonitor hepatic function, think DIs---potent inhibitor
Zyflo CR will be given BID instead of QID. But patients will still need liver function tests every month for the first 3 months...then every 2 to 3 months for the rest of the first year. – 2007
Omalizumab. Save the monoclonal antibody, Xolair, for patients with severe asthma and allergies...who are not responding adequately to high-dose inhaled steroids and long-acting beta-agonists.
New NIH guidelines will improve asthma treatment. You'll see renewed emphasis on controlling symptoms...patient education...and avoiding allergens.
Zyflo CR will be given BID instead of QID. But patients will still need liver function tests every month for the first 3 months...then every 2 to 3 months for the rest of the first year. – 2007
Omalizumab. Save the monoclonal antibody, Xolair, for patients with severe asthma and allergies...who are not responding adequately to high-dose inhaled steroids and long-acting beta-agonists.
New NIH guidelines will improve asthma treatment. You'll see renewed emphasis on controlling symptoms...patient education...and avoiding allergens.
PG 142
Drugs for the Treatment of AsthmaDrugs for the Treatment of Asthma
CorticosteroidsCorticosteroids
Inhalational; reduce inflammation and bronchial reactivity; may Inhalational; reduce inflammation and bronchial reactivity; may cause oral candidiasis, cough, and other steroid effects (with cause oral candidiasis, cough, and other steroid effects (with prolonged use). Prophylaxis only.prolonged use). Prophylaxis only.
•• Beclomethasone dipropionate (Beclovent, Vanceril)Beclomethasone dipropionate (Beclovent, Vanceril)
• • Triamcinolone acetonide (Azmacort)Triamcinolone acetonide (Azmacort)
• • Flunisolide (Aerobid)Flunisolide (Aerobid)
• • Fluticasone propionate (Flovent)Fluticasone propionate (Flovent)
• • Mometasone (Asmanex Twisthaler)Mometasone (Asmanex Twisthaler)
• • Budesonide (Pulmicort) (Pulmicort Respules – only neb Budesonide (Pulmicort) (Pulmicort Respules – only neb ICS)ICS)
AnticholinergicsAnticholinergics
Ipratropium bromide (Atrovent); bronchodilator. Reduces Ipratropium bromide (Atrovent); bronchodilator. Reduces secretions; alternative to beta-2 agonists; anticholinergic secretions; alternative to beta-2 agonists; anticholinergic adverse effectsadverse effects
- combivent – albuterol and ipratropium- combivent – albuterol and ipratropium
Tiotropium (Spiriva)----long acting, dry powder capsule for Tiotropium (Spiriva)----long acting, dry powder capsule for inhalationinhalation
PG 143
Drugs for the Treatment of AsthmaDrugs for the Treatment of Asthma
Mast cell stabilizersMast cell stabilizers
Anti-inflammatory; very safe; for prophylaxis onlyAnti-inflammatory; very safe; for prophylaxis only
• • Cromolyn sodium (Intal, Nasalcrom)Cromolyn sodium (Intal, Nasalcrom)
• • Nedocromil sodium (Tilade)Nedocromil sodium (Tilade)
Combination productsCombination products
Ipratropium bromide/albuterol sulfate (Combivent)Ipratropium bromide/albuterol sulfate (Combivent)
Salmeterol xinafoate/fluticasone propionate (Advair Salmeterol xinafoate/fluticasone propionate (Advair Diskus)Diskus)
SymbicortSymbicort contains the corticosteroid budesonide ( contains the corticosteroid budesonide (PulmicortPulmicort)...plus the )...plus the long-acting beta-agonist formoterol (long-acting beta-agonist formoterol (ForadilForadil). - 2007 - 2 puffs BID ). - 2007 - 2 puffs BID
Side effects of oral corticosteroids include all of the following except:
a. hyperglycemia
b. nervousness
c. fluid retention
d. HPA axis suppression
e. thrombocytopenia
Side effects of oral corticosteroids include all of the following except:
a. hyperglycemia
b. nervousness
c. fluid retention
d. HPA axis suppression
e. thrombocytopenia
Side effects of oral corticosteroids include all of the following except:
a. hyperglycemia
b. nervousness
c. fluid retention
d. HPA axis suppression
e. thrombocytopenia
Side effects of oral corticosteroids include all of the following except:
a. hyperglycemia
b. nervousness
c. fluid retention
d. HPA axis suppression
e. thrombocytopenia
Patients exhibiting Cushing syndrome should avoid products containing:
a. corticosteriods
b. iodine
c. sulfas
d. penicillins
e. salicylates
Patients exhibiting Cushing syndrome should avoid products containing:
a. corticosteriods
b. iodine
c. sulfas
d. penicillins
e. salicylates
Patients exhibiting Cushing syndrome should avoid products containing:
a. corticosteriods
b. iodine
c. sulfas
d. penicillins
e. salicylates
Patients exhibiting Cushing syndrome should avoid products containing:
a. corticosteriods
b. iodine
c. sulfas
d. penicillins
e. salicylates
Which of the following drugs is/are administered by dry powder inhalation?
I. Ipratropium (atrovent of combivent)II. Pirbuterol (MaxAir Turboinhaler)III. Salmeterol (Diskus)
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Which of the following drugs is/are administered by dry powder inhalation?
I. Ipratropium (atrovent of combivent)II. Pirbuterol (MaxAir Turboinhaler)III. Salmeterol (Diskus)
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Which of the following drug(s) is/are administered by dry powder inhalation?
I. Ipratropium (atrovent of combivent)II. Pirbuterol (MaxAir Turboinhaler)III. Salmeterol (Diskus)
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
Which of the following drug(s) is/are administered by dry powder inhalation?
I. Ipratropium (atrovent of combivent)II. Pirbuterol (MaxAir Turboinhaler)III. Salmeterol (Diskus)
a. I onlyb. III onlyc. I and II onlyd. II and III onlye. I, II, and III
All of the following drugs are available as aerosol units EXCEPT:
a. Spiriva
b. Azmacort
c. Rhinocort
d. Beconase
e. Combivent
All of the following drugs are available as aerosol units EXCEPT:
a. Spiriva
b. Azmacort
c. Rhinocort
d. Beconase
e. Combivent
All of the following drugs are available as aerosol units EXCEPT:
a. Spiriva
b. Azmacort
c. Rhinocort
d. Beconase
e. Combivent
All of the following drugs are available as aerosol units EXCEPT:
a. Spiriva
b. Azmacort
c. Rhinocort
d. Beconase
e. Combivent
Drugs Used to Treat Glaucoma
Drugs Used to Treat Glaucoma
NAPLEX
PG 136
Causes of GlaucomaCauses of Glaucoma
• • Wide or open angle – most common, malfunction of trabecular Wide or open angle – most common, malfunction of trabecular meshworkmeshwork
• • Narrow angle or closed angle – Narrow angle or closed angle – obstruction of the outflowobstruction of the outflow of of aqueous humor through the trabecular meshwork.aqueous humor through the trabecular meshwork.
An instrument used to measure intraocular pressure is a(n):
a. gonioscope
b. otoscope
c. ophthalmoscope
d. tonometer
e. barometer
An instrument used to measure intraocular pressure is a(n):
a. gonioscope
b. otoscope
c. ophthalmoscope
d. tonometer
e. barometer
An instrument used to measure intraocular pressure is a(n):
a. gonioscope (lens to study angle of eye)
b. otoscope (instrument to examine the drum membrane of the ear)
c. ophthalmoscope (device to study interior of eye)
d. tonometer (device to measure intraocular pressure)
e. barometer (device to measure the atmospheric pressure)
An instrument used to measure intraocular pressure is a(n):
a. gonioscope (lens to study angle of eye)
b. otoscope (instrument to examine the drum membrane of the ear)
c. ophthalmoscope (device to study interior of eye)
d. tonometer (device to measure intraocular pressure)
e. barometer (device to measure the atmospheric pressure)
PG 136
Drugs for Glaucoma TreatmentDrugs for Glaucoma Treatment
Goal of Therapy – reduced intraocular pressure (IOP)Goal of Therapy – reduced intraocular pressure (IOP)
- measured by a tonometer (10-20mmhg)- measured by a tonometer (10-20mmhg)
- decrease rate of aqueous humor production- decrease rate of aqueous humor production
- increase rate of outflow (drainage) of aqueous - increase rate of outflow (drainage) of aqueous
humor humor
SympathomimeticsSympathomimetics— — increase outflow and decrease increase outflow and decrease production of aqueous humorproduction of aqueous humor
- epinephrine (Epifrin, Glaucon) – discard if color change - epinephrine (Epifrin, Glaucon) – discard if color change occurs occurs
- dipiverfrin (Propine) – epinephrine prodrug – less side - dipiverfrin (Propine) – epinephrine prodrug – less side effectseffects
- apraclonidine (Iopidine) – alpha-2 agonist; - apraclonidine (Iopidine) – alpha-2 agonist; watch for watch for ocular ocular allergy allergy
- brimonidine (Alphagan) - - brimonidine (Alphagan) - alpha-2 agonist, alpha-2 agonist, more selectivemore selective
PG 136
Drugs for Glaucoma TreatmentDrugs for Glaucoma TreatmentMiotics (direct acting)—Miotics (direct acting)—have direct have direct cholinergic actioncholinergic action causing causing miosis; increases outflow, may cause eye pain, burning, blurred vision; miosis; increases outflow, may cause eye pain, burning, blurred vision; less with gel and Ocusert formulationsless with gel and Ocusert formulations
- acetylcholine (Miochol)- acetylcholine (Miochol)
- carbachol (Isoptocarbachol)- carbachol (Isoptocarbachol)
- - Pilocarpine (Isoptocarpine, Pilocar, Pilostat, Pilopine HS, Pilocarpine (Isoptocarpine, Pilocar, Pilostat, Pilopine HS, Ocusert Pilo)Ocusert Pilo)
Miotics (cholinesterase inhibitors)—Miotics (cholinesterase inhibitors)—increase cholinergic action by increase cholinergic action by inhibiting cholinesterase; similar adverse effects as direct-acting inhibiting cholinesterase; similar adverse effects as direct-acting mioticsmiotics
- physostigmine (Eserine) – may cause cataracts- physostigmine (Eserine) – may cause cataracts
- Demecarium (Humersol)- Demecarium (Humersol)
- Echothiophate (phospholine iodide)- Echothiophate (phospholine iodide)
mydriasismydriasis
PG 136
Drugs for Glaucoma TreatmentDrugs for Glaucoma TreatmentBeta-adrenergic blocking agentsBeta-adrenergic blocking agents — — reduce production of aqueous reduce production of aqueous humor; watch for possible breathing difficulty, bradycardia, humor; watch for possible breathing difficulty, bradycardia, hypotension, and CNS depressionhypotension, and CNS depression
- betaxolol (Betopic, Betoptic S) – beta 1 selective- betaxolol (Betopic, Betoptic S) – beta 1 selective
- levobetaxolol (Betaxon) – beta 1 selective- levobetaxolol (Betaxon) – beta 1 selective
- carteolol (Ocupress), levobunolol (Betagan, AKBeta)- carteolol (Ocupress), levobunolol (Betagan, AKBeta)
- metipranolol (Optipranolol), - metipranolol (Optipranolol),
- timolol (Timoptic, Timoptic XE) - timolol (Timoptic, Timoptic XE) B1 & B2B1 & B2
Prostaglandin analogsProstaglandin analogs — — increase outflow of aqueous humor; may increase outflow of aqueous humor; may darken iris color and cause thickened lashesdarken iris color and cause thickened lashes
- latanoprost (Xalatan)- latanoprost (Xalatan)
- bimatoprost (Lumigan)- bimatoprost (Lumigan)
- travoprost (Travatan)- travoprost (Travatan)
- Unoprostone (Rescula) - Unoprostone (Rescula) Not available in U.S.Not available in U.S.
PG 136
Drugs for Glaucoma TreatmentDrugs for Glaucoma Treatment
Carbonic anhydrase inhibitorsCarbonic anhydrase inhibitors — — suppress production of aqueous suppress production of aqueous humor; watch for urinary frequency and nephrolithiasishumor; watch for urinary frequency and nephrolithiasis
- dichlorphenarnide (Daranide)- dichlorphenarnide (Daranide)
- acetazolamide (Diamox)----oral capsules, IV – - acetazolamide (Diamox)----oral capsules, IV – Also used for Also used for mountain sicknessmountain sickness
- methazolamide (Neptazane)- methazolamide (Neptazane)
- dorzolamide (Trusopt)- dorzolamide (Trusopt)
- brinzolamide (Azopt) - brinzolamide (Azopt)
Osmotic diuretics----given orally or IVOsmotic diuretics----given orally or IV
-- glycerin (Osmoglyn) , mannitol (Osmitrol)glycerin (Osmoglyn) , mannitol (Osmitrol)
- urea (Ureaphil), isosorbide (Isomotic)- urea (Ureaphil), isosorbide (Isomotic)
Timoptic dosage forms include:I. capsule
II. tablet
III. ophthlamic solution
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Timoptic dosage forms include:I. capsule
II. tablet
III. ophthlamic solution
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Timoptic dosage forms include:I. capsule
II. tablet
III. ophthlamic solution
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Timoptic dosage forms include:I. capsule
II. tablet
III. ophthlamic solution
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Dosage forms for timolol maleate include:I. gel
II. tablet
III. ophthlamic solution
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Dosage forms for timolol maleate include:I. gel
II. tablet
III. ophthlamic solution
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Dosage forms for timolol maleate include:I. gel
II. tablet
III. ophthlamic solution
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Dosage forms for timolol maleate include:I. gel
II. tablet
III. ophthlamic solution
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Glaucoma Case StudyGlaucoma Case Study
Page 138Page 138
Pilocarpine can be classified as a(n):
a. anticholinergic agent
b. carbonic anhydrase inhibitor
c. beta-adrenergic blocking agent
d. cholinergic agent
e. sympathomimetic agent
Pilocarpine can be classified as a(n):
a. anticholinergic agent
b. carbonic anhydrase inhibitor
c. beta-adrenergic blocking agent
d. cholinergic agent
e. sympathomimetic agent
Pilocarpine can be classified as a(n):
a. anticholinergic agent
b. carbonic anhydrase inhibitor
c. beta-adrenergic blocking agent
d. cholinergic agent
e. sympathomimetic agent
Pilocarpine can be classified as a(n):
a. anticholinergic agent
b. carbonic anhydrase inhibitor
c. beta-adrenergic blocking agent
d. cholinergic agent
e. sympathomimetic agent
An Ocusert Pilo-20 system:
a. is administered orally once daily
b. releases 20 mg of pilocarpine each day
c. must be replaced each month
d. releases 20 µg of pilocarpine each hour
e. must be soaked in normal saline just prior to use
An Ocusert Pilo-20 system:
a. is administered orally once daily
b. releases 20 mg of pilocarpine each day
c. must be replaced each month
d. releases 20 µg of pilocarpine each hour
e. must be soaked in normal saline just prior to use
An Ocusert Pilo-20 system:
a. is administered orally once daily
b. releases 20 mg of pilocarpine each day
c. must be replaced each month
d. releases 20 µg of pilocarpine each hour
e. must be soaked in normal saline just prior to use
An Ocusert Pilo-20 system:
a. is administered orally once daily
b. releases 20 mg of pilocarpine each day
c. must be replaced each month
d. releases 20 µg of pilocarpine each hour
e. must be soaked in normal saline just prior to use
A normal intraocular pressure reading would be:
a. 10-20 mm Hg
b. 20-30 mm Hg
c. 30-40 mm Hg
d. 40-50 mm Hg
e. 50-60 mm Hg
A normal intraocular pressure reading would be:
a. 10-20 mm Hg
b. 20-30 mm Hg
c. 30-40 mm Hg
d. 40-50 mm Hg
e. 50-60 mm Hg
A normal intraocular pressure reading would be:
a. 10-20 mm Hgb. 20-30 mm Hg c. 30-40 mm Hg d. 40-50 mm Hg e. 50-60 mm Hg
A normal intraocular pressure reading would be:
a. 10-20 mm Hgb. 20-30 mm Hg c. 30-40 mm Hg d. 40-50 mm Hg e. 50-60 mm Hg
Special caution must be used when timolol is used in patients with:
a. sulfonamide allergyb. asthma c. cancer d. hypertension e. NSAID hypersensitivity
Special caution must be used when timolol is used in patients with:
a. sulfonamide allergyb. asthma c. cancer d. hypertension e. NSAID hypersensitivity
Special caution must be used when timolol is used in patients with:
a. sulfonamide allergyb. asthma c. cancer d. hypertension e. NSAID hypersensitivity
Special caution must be used when timolol is used in patients with:
a. sulfonamide allergyb. asthma c. cancer d. hypertension e. NSAID hypersensitivity