Dr. M . BercovitchDr. M . Bercovitch

Hospice Tel HaShomer

PURPOSEPURPOSE

TO PRESENT A SELECTION OF VARIOUS ANALGESIC DRUGS

AND ADJUVANTS USEFUL IN PAIN CONTROL

THE CATEGORIES OF DRUGS USEFULTHE CATEGORIES OF DRUGS USEFUL

IN CHRONIC PAIN TREATMENTIN CHRONIC PAIN TREATMENT

ANALGESICS

ADJUVANTS

CLASSIFICATION OF ANALGESICSCLASSIFICATION OF ANALGESICS

ACCORDING TO THE INTENSITY OF PAINACCORDING TO THE INTENSITY OF PAIN

ANALGESICS FOR MILD PAIN

ANALGESICS FOR MODERATE PAIN

ANALGESICS FOR SEVERE PAIN

ANALGESICS FOR MILD PAIN

ACID ACETYL SALICILIC

PARACETAMOL

OTHER NSAIDs

ACID ACETYL SALICILIC

Aspirin, Cartia, Micropirine,….

Mechanism of action: INHIBITING THE SYNTHESIS OF PGE2

Pharmacology: ABSORBED RAPIDLY, PEAK SERUM LEVELS - 2hours

THE ONSET OF ACTION AFTER 5-30min

A SINGLE ORAL DOSE IS EFFECTIVE FOR 4-6 hours

BIOTRANSFORMED IN THE LIVER AND EXCRETED IN THE URINE

Indications In PC: MILD TO MODERATE PAIN ( STEP 1 OF THE WHO LADDER)

PANCREATIC AND HEAD & NECK CANCERS

CI: ULCER BLEEDING DYSCRASIAS, URTICARIA,

Caution in MULTIPLE MYELOMA AND RENAL FAILURE

HAS CEILLING EFFECT

CAUSES IRREVERSIBLE IMPAIRMENT OF PLATELET FUNCTION

ACID ACETYL SALICILIC

Incompatibility: REDUCES DIURETIC ACT OF SPIRONOLACTONE (70%)

ADDITIVE EFFECTS WITH ANTICOAGULANTS

How supplies: TB- 85mg, 100mg, 500mg

ENTERIC COATED TB:325mg, 500mg

SUPPOSITORIES:500mg

Dosage & Administration 650mg- 1000mg q6h

Adverse & side effects: GASTRITIS & UPPER GI BLEEDING

PLATELET FUNCTION BLEEDING TIME

OTHER NSAIDs

Mechanism of action: INHIBIT THE CYCLO - OXYGENASE ENZIME THEREBY

REDUCING TISSUE LEVELS OF PROSTAGLANDINS

TWO GROUPS: COX-1 AND COX-2

Pharmacology: ABSORBED IN THE GI TRACT, METABOLIZED IN THE LIVER,EXCRETED IN THE URINE.ONSET OF ANALGESIC ACTION - 30-60 min

PEAK ANALGESIC EFFECT: 1-2 hours

Indications in PC: BONE PAIN

MILD TO MODERATE VISCERAL PAIN

CI:ACTIVE PEPTIC ULCER, RECCENT HYSTORY OF GI BLEEDING

CAUTION IN MULTIPLE MYELOMA

RENAL IMPAIRMENT OR PRERENAL FAILURE

HEART FAILURE

OTHER NSAIDs

Adverse side effects: PERIPHERAL EDEMA, FLUID RETENTION

DYSPEPSIA, NAUSEA, EPIGASTRIC PAIN, GI BLEEDING,

CONSTIPATIONPROLONGATION OF BLEEDING TIME

PRURITUS, RASH

Incompatibility: with: ANTICOAGULANTSOTHER DRUGS THAT INHIBIT PLATELET AGGREGATION

CARBPENICILLINE, PIPERACILLINE, VALPORIC AC, OTHER NSAIDs

POTENTIATE THE ACTIVITY OF HYPOGLICEMIC AG

MAY DECREASE THE EFFECTIVENESS OF DIURETICS

OTHER NSAIDs

How Supplied And Dosages: NAPROXEN - NAXYN- 250, 500mg, 1000mg

Dose : 250-500mg PO bid

DICLOFENAC - VOLTAREN- 25mg, 100mg

ARTHROTEC 50* - 50mg +misoprostol 200mcg

Dose: 1Tb PO bid, tid

Dose:1-2 tb daily

NIMESULID - MESULID - 100mgDose: 100mg- 200mg PO bid

NABUMETONE - RELIFEX - 500mg

Dose: 1000mg-2000mg PO/day

CELECOXIB - CELEBRA - 100ngDose 100mg PO/day

IBUPROFEN- ADEX - 200mg; 400MG

Dose 200mg - 400mg TID

ETORICOXIB –ARCOXIA- 60mg; 90mg;120mgDose: 60mg-120mg once daily

ETODOLAC- ETOPAN – 200mg;300mg;400mgETOPAN XL 600mg

Dose: 200-400mg tid 600mg bid

LORNOXICAM – XEFO – 8mgDose 8mg once twice daily

OTHER NSAIDs

ANALGESICS FOR MODERATE PAIN

CODEINETRAMADEX

COMBINATION OF LOW DOSE OF STRONG OPIOID WITH PARACETAMOL / ASPIRIN

PERCODAN

PERCOCET

LOW DOSE OF STRONG OPIOD

OXYCODONE

MORPHINE

TRAMADEX

TRAMADOL HCl

Indications in PC: MODERATE TO SEVERE PAIN

Mechanism of action: CENTRALLY, INVOLVED IN BINDING TO MU-RECEPTORS AND

INHIBITION OF REUPTAKE OF NOREPINEPHRINE AND

SEROTONINE

CI: INCREASED INTRACRANIAL PRESSURE,

IMPAIRMENT OF RENAL AND HEPATIC FUNCTION

Side effects: SWEATING, DIZINESS, NAUSEA, VOMITING DRY MOUTH

Interaction With Other Drugs: OTHER DRUGS ACTING ON THE CNS, MAO INHIBITORS

CARBAMAZEPINE SERUM CONC OF TRAMADOL

How Supplied And Dosages: Tb TRAMADEX - 100mg

Dose: 100mg - 200mg, ONCE OR bid

DROPS: 10 - 20 every 4,6,8, hours

10drops =25mg TRAMADOL

FLASHTAB:=50mg-100mg every 4-6 hours

PERCODAN5mg OXYCODONE + ASPIRINE

PERCOCET

5mg OXYCODONE + PARACETAMOL

OXYCODONE

MORPHINE

ANALGESICS FOR SEVERE PAIN

OXYCODONE

MORPHINE

FENTANYL

METHADONE

OXYCODONE

OXYCONTIN, OXY-COD

PERCOCET, PERCODAN

Mechanism of action: IS BINDING TO KAPPA RECEPTORS

HAS NO CEILLING EFFECT

HAS NO ACTIVE METABOLITS

HAS NO LIVER AND RENAL TOXICITY

ACTIVE AFTER 50 min

PROVIDE ANALGESIA FOR 12 hours

STEADY STATE WITHIN 24 hours

HAS A SHORT HALF LIFE - 5 hours

Pharmacology: METABOLIZED IN THE LIVER AND EXCRETED BY THE KIDNEYS

SEMISYNTHETIC NARCOTIC ANALGESIC

OXYCODONE

Indications in PC: MODERATE PAIN AS PERCODAN & PERCOCET

SEVERE PAIN AS OXYCONTIN

BONE PAIN

CI: CORELATED TO ASPIRINE SIDE EFFECTS

Adverse side effects: DROWSINESS, CONSTIPATION, NAUSEA & VOMITING

Incompatibility: MAO INHIBITORS, ANTIDEPRESSANTS, ANTICHOLINERGICSADDITIVE EFFECTS with other CNS DEPRESSANTS

OXYCODONE

How supplied: Tb OXYCONTIN - CONTROLLED RELEASE 10ng, 20mg, 40mg, 80mg. Syr OXYCOD 50ml

Dosage & Administration: OXYCONTIN - REGULAR 12 hourly SCHEDULE

DOSAGES AS NECESSARY BEGINNING FROM 10mgUNTIL THE NECESSARY DOSE TO ACHEVE ANALGESIA

OXYCOD -IMMEDIATE RELEASE (20-30min)

INDICATED FOR BREAKTHROUGH PAIN

TITRATION

INCIDENTAL PAIN

INDICATED TO TAKE 1 hour BEFORE ACTIVITY

DOSE: 2mg/ml

MORPHINE

MORPHINE, MCR,MCR UNO,MIR

Mechanism of action: ACTIVATES MU & KAPPA RECEPTORS

GIVEN BY INHALATIONS ACT LOCALLY ON SPECIFIC

ENDORPHINE RECEPTORS IN THE LUNG - ONLY

5% REACHES THE CIRCULATION

Pharmacology:ABSORBED BY THE GI TRACTUS, RECTAL MUCOSA, AFTER SQ & IM

BIOAVAILABILITY - 25%

ONSET OF ACTION AFTER ORAL ADM - 15-60min FOR MIR

60- 90min MCR

PEAK EFFECT 30 -60min MIR

1- 4 h MCR

DURATION OF ACTION 2-7 h MIR6-12 h MCR

15-30min SQ

50-90min SQ

2-7 h SQ

ONLY SMALL QUANTITIES PASS THE BOOD BRAIN BARRIER

MORPHINE

Indications in PC: SEVERE PAIN

GIVEN BY NEBULIZER RELIEVE PERSISTENT COUGH & DYSPNEEA

GIVEN IV RELIEVE AC. PULMONARY EDEMA

Contraindications: NONE

CAUTION IN SEVERE RENAL INSSUFICIENCY (M6G)

HEPATIC FAILLURE

Incompatibility: CIMENTIDINE -MO TOXICITY

PHENOTIAZINES - ADDITIVE SEDATIVE EFFECT

MORPHINE

How supplied: SHORT ACTING-Tb MIR 15mg, 30mg

LONG ACTING - MCR - 10mg, 30mg, 100mg, 200mG

MCR UNO 30mg, 60mg, 120mg, 200mg

Dosage & Administration:DOSSAGE TITRATION q4 h +PRN UNTIL PAIN CONTROL

THE TOTAL MO REQUIREMENTS /24 h WILL BE DIVIDED BY 2

SUBSEQUENTLY MIR IS USED ONLY AS RESCUE DOSE

MAX MAINTENANCE DOSE “THE SKY IS THE LIMIT”

A LAXATIVE REGIMEN SHOULD BE STARTED

BY NEBULIZER START WITH 10mg - 100mg

FENTANYLDURAGESIC

Mechanism of action: SYNTHETIC OPIOID ANALGESIC

ACTIVATES MU & KAPPA RECEPTORS

ACTS ALSO DIRECTLY ON SMOOTH MUSCLE OF THE

GI TRACT TO INCREASE THE TONE AND DECREASE

PROPULSIVE CONTRACTIONS

Pharmacology: CONTINUOUS SYSTEMIC DELIVERY FOR 72h

ONSET OF ACTION IS GRADUAL 12-24 h BEFORE THE PLASMA

LEVEL REACH A STEADY STATE.

PEAK SERUM LEVELS 24-72 h AND DECLINE GRADUALLY

FAILLING 50% IN 13-22h

CLEARANCE MAY BE REDUCED IN GERIATRIC PATIENTS

METABOLIZED IN THE LIVER AND EXCRETED IN THE URINE

FENTANYL

Indications in PC: SEVERE PAIN, IN THOSE UNABLE TO TAKE ORAL MEDICATION

STABLE REQUIREMENTS OF OPIOIDS

CI: SENSITIVTY TO FENTANYL OR ADHESIVES

Incompatibility: OTHER CNS DEPRESSANTS - MAY PRODUCE ADDITIVE

DEPRESSIVE EFFECTS

How Supplied: PATCHES CONTAINING 25mcg/h, 50mcg/h, 75mcg/h, 100mcg/h.

FENTANYL

Dosage & Administration:: TITRATE WITH VARIOUS FORMS OF MORPHINE

CALCULATE THE TOTAL DOSE NECESSARY FOR 24h

USE THE SIMPLIFIED FORMULA OF”90”

APPLY THE PATCH TO NONIRRITATED SKIN

FOR THE FIRST 24h USE SHORT ACTING MO FOR

GOOD ANALGESIA

USE AS RESCUE DOSES MIR

SOME PATIENTS WILL REQUIRED A NEW PATCH

AFTER 48h

FOR SWITCH START 12-18h AFTER REMOVAL

OF THE PATCH HALF EQUIANALGESIC DOSE OF

ANOTHER OPIOID

ACTIQ(LOLIPOP)

Oral Transmucosal System (OTS™) Drug Delivery Technology

Transcellular:

• Lipophilic

– eg, fentanyl

• Un-ionized

– Molecules readily cross cellular membranes

Paracellular:

• Hydrophilic

– eg, morphine

• Ionized

– Molecules do not cross cellular membranes

• Convenient route of administration

• Favorable safety features (eg, product identification, removal of unit)

ATTRIBUTES OF ACTIQ

• Short consumption time (15 minutes)

• Rapid absorption across buccal mucosa*

• Noninvasive

RELATIVE POTENCY CONSIDERATIONS: ACTIQ TO ORAL MORPHINE1,2

OT fentanyl

IV morphine

Oral morphine

10-20:1

3:1

200 mcg OTFC 2-4 mg IV morphine 6-12 mg oral morph.

Adapted from Lu JK, Bailey PL. [Poster presentation] Presented at the ASA Annual Meeting, October 11-15, 2003, San Francisco, CA. Sevarino FB, et al. Anesth Analg. 1997;84:S330; Lichtor JL et al. Anesth Analg. 1999;89:732-738.

הוספיס

תל השומר

ית ב "פרידמן"

METHADONEADOLAN

PERIPHERAL EFFECTS TO SMOOTH MUSCLE

Mechanism of action: SYNTHETIC OPIOID ANALGESIC

ACTIVATES MU & KAPPA RECEPTORS

Pharmacology: LONGER PLASMA HALF LIFE, ACCUMULATES IN THE TISSUES

CUMMULATIVE TOXICITY

ANALGESIA 6-12h

Indication in PC: ALTERNATIVE MEDICATION IN MO UNRESPONSIVNESS

CI: IN ELDERLY

IN DEMENTED AND DELIRIOUS PATIENTS

METHADONE

Incompatibility: CIMENTIDINE, PHENOTHIAZINES

How Supplied: ORAL SOLUTIONS 5mg/5ml, 10mg/5ml:

Dosage And Administration:START WITH 1/2 TO 2/3 PATIENT’S CURRENT

24h MORPHINE DOSAGE DIVIDED IN

4 DAILY DOSES

AFTER 3 DAYS ELIMINATE ONE DOSE,

AND CONTINUE WITH tid ADMINISTRATION

OPIOID SIDE EFFECTSOPIOID SIDE EFFECTS

SEDATIONSEDATION

CONFUSION, DIZINESSCONFUSION, DIZINESS

NAUSEA AND VOMITINGNAUSEA AND VOMITING

MYOCLONUSMYOCLONUS

CONSTIPATIONCONSTIPATION

ACUTE URINARY RETENTIONACUTE URINARY RETENTION

SWEATINGSWEATING

PRURITUSPRURITUS

OPIOID PRESCRIPTIONOPIOID PRESCRIPTIONגב המרשם

תאריך

שם החולה

מס. הזהות

הכתובת

תרופה

23.05.96

גבי משה לאה

456577895 ,ר”ג5רח’ הנביאים

T. OXYCONTIN 10mg

1 X 2 / d

No 20 tb

עשרים כדורים אוקסיקונטין כל כדור עשרה מ”ג .הכמות ניתן

למשך עשרה יום בלבד

ד”ר מ.ב15555מ.ר.

ONCC A OF B R EA S T

החולה הנ”ל גרה במקום

.מרוחק מבית מרקחת

אנו מבקשים לאשר לה

האםפקת אופיואידים

למשך עשרים יום.

.במד”ר 15555מ.ר

ADJUVANTS ANALGESICSADJUVANTS ANALGESICS

ANTICONVULSANTS - CARBAMAZEPINE (TEGRETOL)

ANTIDEPRESSANTS - AMITRIPTYLINE (ELATROL)

BENZODIAZEPINES - CLONAZEPAM (CLONEX)

BISFOSFONATES - PAMIDRONATE (AREDIA)

ETIDRONATE (ZOMERA)

GABA-AGONISTS - BACLOFEN (LIORISAL)

NMDA ANTAGONISTS - KETAMINE (KETALAR)

STEROIDS

-GABAPENTINE ( NEURONTIN)

נשמח לראותכם!

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מרכז אקדמי

ד”ר מיכאלה ברקוביץ מדריכה מרכזת הוראה

הוספיס תל השומר הוספיס

תל השומר

TEL AVIV UNIVERSITYSACKLER FACULTY OF MEDICINE

SCHOOL OF CONTINUING MEDICAL EDUCATION

- אוניברסיטת תל אביבהפקולטה לרפואה ע”ש סאקלר

בית הספר ללימודי המשך ברפואה

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