Some Spotlights about Pain management
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- 1. By:Ahmed F. El-Sawy,Fourth Year Student, Faculty of
Pharmacy, Alexandria University, Egypt, May 2012.THIS
PRESENTATION:I was awarded The Best Presenter of The Academic Year
2011-2012 for this presentation by the Department of
Pharmaceutics.
- 2. Ahmed El-Sawy, 44078
- 3. Question:6I heard that all analgesics are not safe for
children, pregnant and with breastfeeding, is that true?
- 4. Answer:6 No, not all analgesics are not safe forchildren,
pregnant and with breastfeeding. Butthere are some analgesics
considered as safe.
- 5. Pregnant &Children breastfeeding Non-opioid Aspirin
analgesics Paracetamol Paracetamol NSAIDs NSAIDs Aspirin
- 6. Children Paracetamol safe. NSAIDs useful. Ibuprofen 2 years.
Naproxen 12 years. Ketoprofen 16 years. Aspirin restricted. Opioids
severe pain.Pregnant Paracetamol safe. Aspirin restricted.
{Exception?} Opioids restricted. NSAIDs contraindicated during 3rd
trimester.Breastfeeding Paracetamol safe. Aspirin restricted.
Ibuprofen compatible. Naproxen compatible.
- 7. Choice of analgesics in Children: Non-opioid analgesics are
used in infants and children either alone for minor pain or as an
adjunct to opioid analgesics in severe pain (they can reduce opioid
requirements perhaps by up to 40% => "opioid dose-sparing"
effect.). Paracetamol is frequently used but it lacks any
anti-inflammatory effect.
- 8. NSAIDs such as ibuprofen are useful for minor painespecially
when associated with inflammation ortrauma. NSAID Child Age
Ibuprofen [OTC ] > 2 years Naproxen [OTC] > 12 years
Ketoprofen [OTC] > 16 yearsAspirin is greatly restricted due to
its associationwith Reyes syndrome. (children under 16 years)
- 9. Children severe pain: Opioids ((POM))1. Opioid agonists:
(weak opioids & strong opioids)Weak codeine(1st choice weak
opioid) & hydrocodone.Strong morphine, hydromorphine &
fentanyl.N.B: codeine is demethylated by LMEs to the active
morphine, so LME-inhibitors (e.g. quinidine & fluoxetine) can
abolish its metabolic activation and activity.2. Opioid partial
agonists: pentazocine & buprenorphine.N.B: tramadol (strong
centrally acting analgesic with antidepressant activity) used as
antidepressant & NOT in acute pain due to high risk of nausea
& vomiting.3. Opioid antagonists: naloxone; for opioid
intoxication.N.B: Dependence, N, V, C, resp. depression, sedation
& tolerance are opioids adverse effects.
- 10. Adjuvant analgesicsAre drugs with weak or no analgesic
action alone, but enhance the action of analgesics when co-
administered with them. Antidepressants (TCA: amitriptyline &
desipramine). Anticovulsants (Gabapentin, pregabalin &
carbamazepine). Topical: lidocaine & capsaicin-OTC. Sk. M.
relaxants: Dantroline sod. is the only peripheral acting directly
on muscles (less side effects).
- 11. Choice of analgesics inPregnant and Breastfeeding: Aspirin
is classified as FDA pregnancy category C ( adverse effects on
animals & no controlled human studies ) risk during Trimesters
1 and 2 and category D ( positive evidence of human fetal risk )
during Trimester 3. Salicylates are excreted in breast milk.Aspirin
should be avoided during pregnancy {Exceptions??} and while
breast-feeding.
- 12. AspirinPregnancy 1. impaired platelet function
(haemorrhage). 2. delayed onset and increased duration of labour
(increased blood loss). 3. with high doses, closure of fetal ductus
arteriosus in utero and possibly persistent pulmonary hypertension
of newborn. 4. kernicterus in jaundiced neonatesBreast-
avoidpossible risk of Reyes syndrome; regularfeeding use of high
doses could impair platelet function and produce
hypoprothrombinaemia in infant if neonatal vitamin K stores
low.
- 13. =APS=APLS=APLA=Hughes Syndrome=Sticky Blood autoimmune
disorder in which the body recognizes certain normal components of
blood and/or cell membranes as foreign substances and produces
antibodies against them. Patients with these antibodies may
experience blood clots, including heart attacks and strokes, and
miscarriages. There is no cure for APS, but there is treatment. The
treatment of choice for patients with APS who have had a blood clot
is anticoagulant therapy; Aspirin and heparin .
- 14. Paracetamol ( Acetaminophen ) is generally recognized as
the treatment of choice of mild-to-moderate pain.It crosses the
placenta, but considered as safe during pregnancy.It appears in the
breast milk, but considered compatible with breastfeeding.
- 15. NSAIDs , no evidence that they are teratogenic either in
humans or in animals. BUT contraindicated during 3rd trimester of
pregnancy; As they Cause: delayed parturition prolonged labor
increased postpartum bleeding adverse fetal cardiovascular
effectsN.B:Ibuprofen is not excreted in breast milk; so compatible
with breastfeeding.Naproxen is also compatible with
breastfeeding.
- 16. ConclusionChildren Paracetamol safe. NSAIDs useful.
Ibuprofen 2 years. Naproxen 12 years. Ketoprofen 16 years. Aspirin
restricted. Opioids severe pain.Pregnant Paracetamol safe. Aspirin
restricted. Opioids restricted. NSAIDs contraindicated during 3rd
trimester.Breastfeeding Paracetamol safe. Aspirin restricted.
Ibuprofen compatible. Naproxen compatible.
- 17. Question:7Voltaren and Cataflam both containdiclofenac, but
I heard that only Cataflam canbe used by hypertensive patients,
what do youthink?
- 18. Answer:7Voltaren ( contains diclofenac sodium) POM Slower
onset of actionCataflam (contains diclofenac potassium) POM
Immediate-release tablets with rapid onset of action
- 19. Diclofenac According to NOVARTIS: 1. NSAIDs, including
Cataflam , should be used with caution in patients with
hypertension.2. NSAIDs can lead to onset of new hypertension or
worsening of preexisting hypertension, either of which may
contribute to the increased incidence of CV events. Patients taking
thiazides or loop diuretics may have impaired response to these
therapies when taking NSAIDs.3. Blood pressure (BP) should be
monitored closely during the initiation of NSAID treatment and
throughout the course of therapy.
- 20. Effect of dietary sodium Na & H2O intake on blood
retention pressureBlood BloodVolume pressure Cardiac 0utput
- 21. Non-pharmacologic therapy ofhypertension All patients with
prehypertension and hypertension should be prescribed lifestyle
modifications, including(1) weight reduction if overweight(2)
adoption of the Dietary Approaches to Stop Hypertension eating
plan(3) dietary sodium restriction ideally to 1.5 g/day (3.8 g/day
sodium chloride)(4) Regular aerobic physical activity(5) moderate
alcohol consumption (two or fewerdrinks per day)(6) smoking
cessation. Lifestyle modification alone is appropriate therapy for
patients withprehypertension. Patients diagnosed with stage 1 or 2
hypertension shouldbe placed on lifestyle modifications and drug
therapy concurrently.
- 22. Conclusion:
- 23. Question:8Although NSAIDs are used to relieve pain, the
administration of some of their dosage forms might be irritant and
painful. Comment.
- 24. Answer:8Oral dosage forms (tablets, capsules & oral
suspension):GI side effects associated with NSAID use can be both
local and systemic.Local effects occur due to local irritation.
Resolved by lowering the dose, changing to another NSAID, taking an
enteric form of an NSAID and by taking each NSAID dose with food or
a large glass of water.
- 25. Systemic effects can be extremely serious. Regardless of
the route of administration, NSAIDs (with the exception of the
selective or COX-2 inhibiting drugs) interfere with prostaglandin
synthesis throughout the entire body. the patient is at risk of
adverse events such as perforation and hemorrhage of the esophagus,
stomach, and the small or large intestine.
- 26. Patient counseling to GI irritation:1. Dont take an NSAID
with alcohol.2. Dont take more than one type of NSAID, with the
exception of a small daily dose of aspirin for heart attack
prevention.3. Take NSAIDs with a full glass of water or milk, with
meals, or with a prescribed antacid.4. Remain upright 30 minutes
after administration to reduce gastric irritation or ulcer
formation.5. NSAIDs should be used at the lowest effective dose for
the shortest time they are needed.6. Avoid fasting because fasting
can increase toxicity
- 27. Topical dosage forms (gels and creams):The use of topical
NSAIDs gels or creams to treat pain has been reported to cause a
photocontact dermatitis. Most commonly this has occurred with
ketoprofen gel with an incidence of 0.013-0.028/1000. Often the
reaction appears after stopping the application when the skin is
next exposed to sunlight
- 28. Diclofenac-rectal SuppositoryFrom local rectal irritationto
rectal bleeding. (hemorrhoids?)Some NSAID eye drops(irritant)
- 29. Some Parenteral NSAIDs(painful)
- 30. Question:9A patient with history of asthma is suffering
from low back pain, would a NSAID be safe to use?
- 31. Answer:9 various stimuli triggers canOnce asthma develops,
precipitate asthma. Aspirin and NSAIDs are of the asthma triggers.
Handbook of Nonprescription Drugs 16th Ed
- 32. But!!Not all asthmatic patients have the same triggers, and
even for the same patient, his response to a certain particular
trigger changes over time.The mechanism of asthma precipitation
includes degranulation of mast cells and the release of histamine
and leukotrienes that cause severe bronchoconstriction.Asthmatic
patients should be cautious about the use of NSAIDs !!!!
- 33. Why should asthmatic patient be cautious about the use of
NSAIDs?Because of increased risk of aspirin sensitivity; 4% of
asthmatic patients have this problem( Severe life- threatening
symptoms from rashes, nasal congestion, cough, worsening asthma to
anaphylaxis ).And there is a significant potential for cross-
sensitivity to other NSAIDs such as ibuprofen and naproxen.
- 34. Role of the pharmacist & patient counseling: The
pharmacist can check if a person with asthma has used aspirin or
ibuprofen before. If they have done so without problems, they can
continue. For sensitive patients, they should be cautioned to:1.
Check the labels of headache and pain relief medications to see if
they contain any NSAIDs.2. Avoid any other agents that contain
salicylates such as oil of wintergreen.
- 35. Question:10A young woman is suffering severe abdominal pain
diagnosed as primary dysmenorrhea. How should this menstrual pain
be treated?
- 36. Answer:10Primary dysmenorrhoea:classically presents as a
cramping lowerabdominal pain that often begins during the day
before bleeding starts.The pain gradually eases after the startof
menstruation and is often gone by theend of the first day of
bleeding.N.B: Secondary dysmenorrhea occurs one week before
menstruation. pain may get worse once bleeding starts or during
sexual intercourse.
- 37. MedicationThe Cause of the pain of dysmenorrhoea:is thought
to be due to prostaglandin (PG-2 ) activity. the use of analgesics
thatinhibit the synthesis of prostaglandins is logical. BUTThe
pharmacist has to make sure that the patient is not already taking
an NSAID.
- 38. CautionWhen to refer to the doctor1. Presence of abnormal
vaginal discharge2. Abnormal bleeding3. Symptoms suggest secondary
dysmenorrhea4. Severe intermenstrual pain and bleeding5. Failure of
medication6. Pain with a late period (possibility of an ectopic
pregnancy)7. Presence of fever
- 39. Management1. Simple explanation2. sympathy3. reassurance.4.
Treatment with simple analgesics is often very effective in
dysmenorrhoea.
- 40. TreatmentsIbuprofen Hyoscine Caffeine (DOC) Aspirin
Paracetamol
- 41. 1.Ibuprofen: (drug of choice ):But !!!(take care in case of
previous use of aspirin, and history of GI problems and asthma .)It
inhibits the synthesis of prostaglandin.Dose of 200400 mg three
times daily with maximum daily dose of 1200 mg.A variety of
proprietary brands of ibuprofen is available; Brufen Ibufen
Marcofen
- 42. Caution1) Ibuprofen is contraindicated in case of peptic
ulcer.2) Should be taken with or after food to minimize GI
problems.3) Should not be taken by anyone who is sensitive to
aspirin.4) Should be used with caution in anyone who is asthmatic,
because such patients are more likely to be sensitive to
ibuprofen.The pharmacist can check if a person with asthma has used
ibuprofen before. If they have done so without problems, they can
continue.
- 43. 2. Aspirin: (less effective than Ibuprofen)1. Inhibits the
synthesis of prostaglandins.2. Cause GI upsets and is more irritant
to the stomach.3. In presence of symptoms of nausea and vomiting
with dysmenorrhoea, aspirin is probably best avoided.4. To be taken
with or after meals.
- 44. 3. Paracetamol: (less effective !!! than Ibuprofen and
Aspirin ) : Disadvantages Advantages1. Has little or no 1. Useful
treatment when the effect on the patient cannot take ibuprofen or
aspirin because of stomach levels of problems or potential
prostaglandins. sensitivity.2. Less effective for 2. Useful when
the patient isthe treatment of suffering with nausea and
vomitingdysmenorrhoea. as well as pain, since it does not irritate
the stomach.
- 45. 4. Hyoscine:Smooth muscle relaxant, with antispasmodic
action that reduces cramping.Contraindicated in women with
glaucoma.Contraindicated with tricyclic antidepressants due to
additive anticholinergic effects (dry mouth, constipation, blurred
vision).
- 46. 5. Caffeine: There is some evidence (from a trial comparing
combined ibuprofen and caffeine with ibuprofen alone and caffeine
alone) that caffeine may enhance analgesic effect. Drinking tea,
coffee or cola.
- 47. Clinical11/2003 8/2001 to TrialOral Contraceptives for
Dysmenorrhea in Adolescent GirlsA Randomized Trial Anne Rachel
Davis, MD, Carolyn Westhoff, MD, Katharine OConnell, MD, and Nancy
Gallagher, RN. This trial demonstrated that a low-dose oral
contraceptive was more effective than placebo for moderate or
severe primary dysmenorrhea in adolescents. The improvement in
dysmenorrhea during OC use was consistent across measures.
- 48. References(Questions 6 to 10)1) Handbook of Nonprescription
Drugs, APhA, 16th Edition.2) Symptoms in the Pharmacy: A Guide to
the Management of Common Illness, A. Blenkinsopp, J. Blenkinsopp
and P. Paxton, 5th Edition.3) British National Formulary BNF-61.4)
Australian Pharmaceutical Formulary and Handbook, 21st Edition.5)
Egyptian Drug Guide, 3rd Edition.6) Lippincotts Illustrated
Reviews: Pharmacology, 4th Edition.7) Pharmacotherapy Handbook, 7th
Edition.8) Novartis Cataflam insert.9) FDA drug risk categorization
during pregnancy. http://www.fda.gov10)
www.ConsumerReportsHealth.org/BestBuyDrugs11) Oral Contraceptives
for Dysmenorrhea in Adolescent Girls, A Randomized Trial; Anne
Rachel Davis, MD, Carolyn Westhoff, MD, Katharine OConnell, MD, and
Nancy Gallagher, RN. July, 2005.
- 49. E-mail: ahm.alsawy@yahoo.com Or
ahm.alsawy@facebook.com