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Opioid & Nalokson

NIR dan SHN


MORPHIN
Morphine
(5-4)

General Narcotic agonist-analgesic of opiate receptors:


 Inhibits ascending pain pathways, thus altering response to
pain produces analgesia
 Respiratory depression
 Sedation
 Suppresses cough by acting centrally in medulla

Efek Samping B1-B6 Ada di catatan


Farmakologik  Onset: PO: 15-30 min; IM: 15-30 min; IV: <5 min
 Durasi: IM = IV = 4 jam
 Peak plasma time: PO < 1jam; IM 30-60 min; IV 20 min

Sediaan Injeksi 10 mg/mL


Clinical dosage and use  Dosis Premedikasi: 0.05-0.2 mg/kg IM
 Dosis Analgetik: 0.1-1 mg/kg IV

Warning  Pasien asma dan bronchitis


Drug Interaction  Pasien Hamil
 Gangguan Hepar dan Ginjal
Fentanyl
(3-30)
 Efek analgesic fentanyl 75-125x lebih poten dari morphine

 B1Fentanil tetap berefek depresi ventilasi sama dengan morfin. Fentanil tidak menyebabkan
histamine release (aman utk asma)
 B2 Fentanil tidak menyebabkan vasodilatasi, fentanyl menyebabkan bradikardiaêBP dan
êCO
 B3 Fentanil tetap berefek éICP (despite of unchanged PaCO2). Seizure like activity also in
fentanyl administration.
 B6Skeletal muscle Rigidity
 Onset: IM 7-15 min; IV 3-7 min
 Durasi: IM 1-2 jam; IV 30-60 min
Injeksi 50 mcg/mL
 Dosis premedikasi: 50-100 mcg IM atau slow IV (30-60 menit sebelum bedah)

 Low dose Fentanyl: 1-2 (1-3) mcg/kg IV to provide analgesia


 Fentanyl dose 2-20 mcg/kg (before painful surgical stimulation) blunting circulatory
response to (a) direct laryngoscopy for intubation of the trachea; (b) sudden changes in the
level of surgical stimulation mengurangi kebutuhan analgesia opioid post op
 Dosis besar fentanyl 50-150 mcg/kg untuk induksi anestesi dan pemeliharaan anestesi dengan
kombinasi benzodiazepine dan anestesi inhalasi dosis rendah (pada bedah jantung).

Dosis analgetik pembedahan:


 Minor surgical procedures: 0.5-2 mcg/kg/dose IV
 Major surgery: 2-20 mcg/kg/dose initially; 1-2 mcg/kg/hr maintenance infusion IV;
discontinue infusion 30-60 min prior to end of surgery; limit total fentanyl doses to 10-15
mcg/kg for fast tracking and early extubation
 Adjunct to general anesthesia (rarely used): 20-50 mcg/kg/dose IV
Kombinasi opioid-benzodiazepine efek hypnosis dan depresi ventilasi
Fentanil menurunkan kebutuhan dosis propofol
FENTANYL
Fentanyl
(3-30)
 Efek analgesic fentanyl 75-125x lebih poten dari morphine

 B1Fentanil tetap berefek depresi ventilasi sama dengan morfin. Fentanil tidak
menyebabkan histamine release (aman utk asma)
 B2 Fentanil tidak menyebabkan vasodilatasi, fentanyl menyebabkan bradikardiaêBP dan
êCO
 B3 Fentanil tetap berefek éICP (despite of unchanged PaCO2). Seizure like activity also in
fentanyl administration.
 B6Skeletal muscle Rigidity
 Onset: IM 7-15 min; IV 3-7 min
 Durasi: IM 1-2 jam; IV 30-60 min
Injeksi 50 mcg/mL
 Dosis premedikasi: 50-100 mcg IM atau slow IV (30-60 menit sebelum bedah)

 Low dose Fentanyl: 1-2 (1-3) mcg/kg IV to provide analgesia


 Fentanyl dose 2-20 mcg/kg (before painful surgical stimulation) blunting circulatory
response to (a) direct laryngoscopy for intubation of the trachea; (b) sudden changes in the
level of surgical stimulation mengurangi kebutuhan analgesia opioid post op
 Dosis besar fentanyl 50-150 mcg/kg untuk induksi anestesi dan pemeliharaan anestesi dengan
kombinasi benzodiazepine dan anestesi inhalasi dosis rendah (pada bedah jantung).

Dosis analgetik pembedahan:


 Minor surgical procedures: 0.5-2 mcg/kg/dose IV
 Major surgery: 2-20 mcg/kg/dose initially; 1-2 mcg/kg/hr maintenance infusion IV;
discontinue infusion 30-60 min prior to end of surgery; limit total fentanyl doses to 10-15
mcg/kg for fast tracking and early extubation
 Adjunct to general anesthesia (rarely used): 20-50 mcg/kg/dose IV
Kombinasi opioid-benzodiazepine efek hypnosis dan depresi ventilasi
Fentanil menurunkan kebutuhan dosis propofol
Nalokson
Indications
Reversal of CNS depression and respiratory depression because of suspected opioid
overdose. Unlabeled Use: Opioid-induced pruritus (low dose IV infusion).
Management of refractory circulatory shock.

Action
Competitively blocks the effects of opioids,including CNS and respiratory depression,
without producing any agonist (opioid-like) effects. Therapeutic Effects: Reversal of
signs of opioid excess.
Pharmacokinetics
Absorption: Well absorbed after IM or subcut administration.
Distribution: Rapidly distributed to tissues. Crosses the placenta.
Metabolism and Excretion: Metabolized by the liver. Half-life: 60–90 min (up to 3
neonates).

TIME/ACTION PROFILE (reversal of opioid effects)

ROUTE ONSET PEAK DURATION

IV 1–2min unknown 45min


IM,Subcut 2–5min unknown 45min
Adverse Reactions/Side Effects
CV:VENTRICULAR ARRHYTHMIAS, hypertension, hypotension. GI: nausea, vomiting.

Interactions
Drug-Drug: Can precipitate withdrawal in patients physically dependent on opioid analgesics. Larger
doses may be required to reverse the effects of buprenorphine, butorphanol, nalbuphine, or
pentazocine. Antagonizes postoperative opioid analgesics.