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Pharmacology Conscious Sedation Drugs .. It is yet a matter of selection! Wael Galal; M.D. Anesthesia Consultant KFH Al-Baha
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Pharmacology of sedative drugs (30 08-15)

Jan 10, 2017

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Page 1: Pharmacology of sedative drugs (30 08-15)

Pharmacology Conscious SedationDrugs ..

It is yet a matter of selection!

Wael Galal; M.D.Anesthesia Consultant

KFH Al-Baha

Page 2: Pharmacology of sedative drugs (30 08-15)
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Whipping the patient ..Is it necessary!!

Page 4: Pharmacology of sedative drugs (30 08-15)

My Presentation Objectives!!Beyond reviewing drugs used for conscious sedation

• Which drugs I can choose, for which patient, procedure and under which circumstances?

• How to administer sedation?

• What I can expect to happen?

• What to do when the unexpected happen?(The Rescue Concept)

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• Select your patient• Select for which procedure• Select your agent• Select method(s) of administration• Select sedational circumstances

... Then you master it all.

Pharmacologic Selection

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Which one of these individuals can be given conscious

sedation? … Select for yourself!

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Common Bad Selections for Conscious Sedation

• Obesity and other patients presenting with difficult airway indicators

• Full stomach including those with bleeding varices undergoing EGD maneuvers

• Neglecting the ASA classification (i.e. III or IV)

• Patients with severe cardiorespiratory illness

• Patients with impaired psychologic fitness

• Procedures taking longer than 1-2 hr

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Common Conscious Sedation Procedures

• Endoscopy

• Lumbar puncture

• Wound care

• Minor surgical procedures: simple suturing, dental procedures

• Placement of implanted devices, catheters, and tubes

• Bone marrow aspiration

• Reduction and immobilization of fractures

• Removal of implanted devices and tubes

• Magnetic resonance imaging and computed tomography scan

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The Ideal …Agent!!

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The Ideal Sedating Agent• Predictable onset of

action

• Lack of cumulative effects

• Promote rapid recovery

• Minimal side-effects

• Residual analgesia

• Short duration of action

• Patient safety

• Reversible

• No residual depression

• Painless administration

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Classification• Benzodiapezin

es:– Midazolam– Diazepam

• IV Anesthetics:– Ketamine– Propofol

Benzodiapezines:

– Midazolam(Dormicum)

– Diazepam(Valium)

Opioids:

-Fentanyl-Morphine-Meperidine

(Demerol)

Anesthetics/sedatives:

– Thiopentone(Pentohal)

– Ketamine– Propofol– Dexmedeto-

midine

ALL THESE 3-GROUPS OF DRUGS ARE APPROVED FOR

CONSCIOUS SEDATION; However!!

Page 17: Pharmacology of sedative drugs (30 08-15)

Drug Choice for Conscious Sedation

• This depends on the requirement of:

–Amnesia Midazolam–Analgesia Opiates / Ketamine–Relaxation IV anesthetics/Not

Ketamine–Consciousness Avoid anesthetics

Page 18: Pharmacology of sedative drugs (30 08-15)

ALL SEDATIVES

• Cause Upper Airway Obstruction

• Produce Respiratory Depression

• Blunt Ventilatory Response to – CO2 (main ventilatory drive) and – Oxygen.

Can Do the Following:

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How This Presentation Goes?• Sedation drugs follow two lists (Adult/Pediatric).

• Each Drug has a Dosage instruction to follow, initial bolus increments STOP when a maximum recommended dose is reached.

• Care with age, excretory organ dysfunction and debilitation dosage by 1/3-1/2.

GENERAL RULES

Page 21: Pharmacology of sedative drugs (30 08-15)

• Specific precautions (Mostly patients with CNS dep., Resp. disorders and CVD).

• REMEMBER: our target is Moderate Sedation. Dose-to-effect titration is your tool.

• Sedating agents potentiate the effects of one another (Synergism).

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The Conscious Sedation Sheets (Adults/Pediatric)

Distributed to All Wards

THIS SESSION WILL SIMPLIFY & EXPLAIN

Page 23: Pharmacology of sedative drugs (30 08-15)

Drugs Used for Adult Sedation

Page 24: Pharmacology of sedative drugs (30 08-15)

DRUG Adult Dose ONSET SPECIAL CONSIDERATION

S

REVERSAL AGENT

PRECAUTIONS CONTRAINDICATIONS

& SIDE EFFECTS

MIDAZOLAM(Dormicum)

AnxiolyticSedativeAmnesicAnti-convulsant

Initial dose:1mg. – elderly/debilitated2.5mg. – healthy adultInitial dose should not exceed 2.5mgm.Usual max:Average adult<60 years:5mg. within 30 min.Elderly adult >60 years: 3.5 mg within 30 min.IV Dose rate: 1mg. over 1 min. Wait 2 min. after each increment to fully evaluate effects. Maintain level with 25% of initial IV dose.

Onset: 1 ½-5 min.

Peak: 10-15 min.

Duration: 60-90 min.

Metabolized: liver

Excreted: kidneyRecovery is dose dependent, usually 1-2 hrs.

Reduce dose by 1/3 to 1/2 when used with other CNS depressing drugs or in the elderly or debilitated.Manufacturer recommends not more than 1.5 mgm over at least two minutes in patients with decreased pulmonary reserves.

FLUMAZENIL(Anexate)

P- Elderly/debilitated

C- Hypersensitivity, acute narrow angle glaucoma

S- CNS / Resp. depression- Hypotension- Agitation- N/V, hiccups

DIAZEPAM (Valium)

SedativeAnxiolyticAnti-convulsant

Initial dose: 2mg.Usual Maximum:10-20mg. within 30 mins.Elderly 5-15 mgm. over 30 mins.IV Dose Rate: 2mg. over 3-5 min. Wait 5-10 minutes to evaluate effects.

Onset: 1-5min.

Peak: 2 min.

Duration: 15-60 min.

Metabolized: liver

Excreted: kidney

Administer into large vein

Inject close to IV siteIf additives in IV solution, flush tubing before and after administration.

Never IM

FLUMAZENIL(Anexate)

P- Elderly/debilitated

C- Hypersensitivity-Narrow angle glaucoma- Psychosis

S- CNS / resp. depression- N/V- Hypotension-Dizziness

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Fentanyl

AnalgesiaSedative

Initial Dose:25mcg.-elderly/debilitated25-50 mcg. –healthy adult

Usual Maximum:100-250 mcg. within 30 min.

IV Dose Rate:Administer slowly. Wait 5 minutes to evaluate effect. Maintain level with 25-50% of initial IV dose.

Onset: 1-2 min.

Peak: 3-5 min.

Duration: 30-60 min.

Metabolized: liver

Excreted: kidney

Reduce dose by 1/4 to 1/3when used with other CNS depressing drugs or in the elderly or debilitated.Muscle rigidity from high doses may prevent adequate chest wall expansion and respirations. This is reversed with neuromuscular blockers but patient must be artificially ventilated

Naloxone(Narcan)

P- Elderly/debilitated- Bradyarrhythmias- Head injury- Resp. disease

C-Hpersensitivity

S- CNS/resp. depression- Hypotension- Muscle rigidity- Bradycardia- N/V- Puritus-Seizures

Morphine

AnalgesiaSedative

Initial Dose:2.5mg.-elderly/debilitated5-10 mg. –healthy adult

Usual Maximum:10 mg. within 30 min.

IV Dose Rate:Administer slowly. Wait 5 min. to evaluate effects

Onset: 1 min.

Peak: 15 min.

Duration: 2-4 hrs.

Metabolized: liver

Excreted: kidney

Reduce dose by 1/3 to 1/2 when given with other CNS depressing drugs or in the elderly or debilitated

Naloxone(Narcan)

P- Elderly/debilitated-Respiratory conditions-- Seizure disorders-Head injuryC- Hypersensitivity- Biliary colicS- CNS/resp. depression- Hypotension- N/V-Dizziness

Pethedine(Demerol)

AnalgesiaSedative

Initial dose:25mg.-elderly/debilitated50mg.-healthy adult

Usual Maximum100mg. within 30 min.

IV Dose Rate:Administer slowly. Wait 5 minutes to evaluate effects

Onset: 1 min.

Peak: 5-7 min.

Duration: 2-4 hr.

Metabolized: liver

Excreted: kidney

Reduce dose by 1/3 to 1/2when given with other CNS depressing drugs or in the elderly or debilitated.

Naloxone(Narcan)

P- Elderly/debilitated- SVT- Seizure disorders- Respiratory conditions

C- Hypersensitivity- MAO inhibitors past 14 days

S- CNS/resp. depression- Hypotension- N/V

Page 26: Pharmacology of sedative drugs (30 08-15)

Thiopental (Pentothal)

General anaesthetic agent

Initial dose:50 - 100 mgUsual maximum:3mg/kgIncremental and maximum doses are reduced to 1/3- 1/2 in the elderly.

Onset: 1- 2 min Peak: 4-8 min

Duration of Action: 10 - 30 min

Metabolized: liver

Excreted: kidney

Reduce dose to 1/3 to 1/2when given with other CNS depressing drugs or in the elderly or debilitated.

- S- Hypotension, myocardial depression, CNS and respiratory depression, nausea, vomiting, diarrhea, laryngospasmC- Respiratory conditionsPorphyriasP- Inactive, debilitated, and elderly may be more susceptible to adverse effects. Increased toxicity with other CNS depressants

KETAMINE(Ketalar)

General anaesthetic agent

Initial dose:0.2 - 1.0 mg/kg

Usual maximum:2mg/kg.

Onset: 30 sec. IV 3-4 min. IM

Duration: 5-10 min. IV 12-25 min. IM

Full Recovery: 30-120 minInitial IV dose over 60 sec.(rapid administration may cause respiratory depression)

Antisecretory agent such as atropine (.01mgm/kg) or scopalamine given priorBarbituates and Ketamine should not be injected using the same syringe.Not recommended outside the OR.

- S- Nystagmus,resp. depression, hypersalivation, laryngospasm, non- purposeful movements, emesis, HR,B/P, ICP- “Emergence reaction”- Unpleasant dreams/hallucinations(most common in females>age 10)

C- Hx CV disease or hypertension- Active pulmonary infection or disease- Head injury- Glaucoma or acute globe injury- Psychosis- Conditions with intracranial hypertension- Seizure or CNS disorders- Hx of airway instability, tracheal surgery or stenosis

Propofol (Diprivan)

General anaesthetic agentAnti-emeticAnti-convulsant

Initial dose:10 - 20mg incremental doses every 5 minutes as neededUsual Maximum: 100mg. Give slow IV push to avoid hypotension.

Onset: 30 sec Duration of Action: 10 - 15 min

Reduce dose by 1/3 to 1/2when given with other CNS depressing drugs or in the elderly or debilitated.Restricted to monitored ICU/ED patients and/or use by anesthesia personnel

- S- Respiratory depression, - HR,B/PP- Hx CV disease or hypotension- Active pulmonary infection or disease- Concomitant use with narcotics- Hx of airway instability, tracheal surgery or stenosis

Page 27: Pharmacology of sedative drugs (30 08-15)

Drugs Used for Pediatric Sedation

Page 28: Pharmacology of sedative drugs (30 08-15)

DRUG Pediatric Dose ONSET SPECIAL CONSIDERATIONS

REVERSAL AGENT

PRECAUTIONS CONTRAINDICATIONS

& SIDE EFFECTS

MIDAZOLAM(Dormicum)

AnxiolyticSedativeAmnesicAnti-convulsant

No manufacturer published recommendations

Onset: 1 ½-5 min.Peak: 10-15 min.Duration: 60-90 min.Metabolized: liverExcreted: kidneyRecovery is dose dependent, usually 1-2 hrs.

Reduce dose by 1/3 to 1/2 when used with other CNS depressing drugs or in the debilitated.Manufacturer recommends not more than 1.5 mgm over at least two minutes in patients with decreased pulmonary reserves.

FLUMAZENIL(Anexate)

P- Debilitated

C- Hypersensitivity, acute narrow angle glaucoma

S- CNS / Resp. depression- Hypotension- Agitation- N/V, hiccups

DIAZEPAM (Valium)

SedativeAnxiolyticAnti-convulsant

No manufacturer published recommendationsClinician info:>30 days of age0.25mg/KG over 3 min. Can repeat in 15-30 min. until total of 0.75mg/Kg

Onset: 1-5min.Peak: 2 min.Duration: 15-60 min.Metabolized: liverExcreted: kidney

Administer into large vein

Inject close to IV site

If additives in IV solution, flush tubing before and after administration.

Never IM

FLUMAZENIL(Anexate)

P- Debilitated

C- Hypersensitivity- Narrow angle glaucoma- Psychosis

S- CNS /resp. depression- N/V- Hypotension-Dizziness

Page 29: Pharmacology of sedative drugs (30 08-15)

Fentanyl

AnalgesiaSedative

No manufacturer published recommendations

Onset: 1-2 min.

Peak: 3-5 min.

Duration: 30-60 min.

Metabolized: liver

Excreted: kidney

Reduce dose by 1/4 to 1/3when used with other CNS depressing drugs or in the debilitated.Muscle rigidity from high doses may prevent adequate chest wall expansion and respirations. This is reversed with neuromuscular blockers but patient must be artificially ventilated.

Naloxone(Narcan)

P- Debilitated- Bradyarrhythmias- Head injury- Resp. disease

C-Hpersensitivity

S- CNS/resp. depression- Hypotension- Muscle rigidity- Bradycardia- N/V- Puritus-Seizures

Morphine

AnalgesiaSedative

0.05-0.1mg/kg slowly Onset: 1 min.

Peak: 15 min.

Duration: 2-4 hrs.

Metabolized: liver

Excreted: kidney

Reduce dose by 1/3 to 1/2 when given with other CNS depressing drugs or in the debilitated.

Naloxone(Narcan)

P- Debilitated-Respiratory conditions-- Seizure disorders-Head injury-C- Hypersensitivity-Biliary colic-S- CNS/resp. depression- Hypotension- N/V-Dizziness

Pethedine(Demerol)

AnalgesiaSedative

1-2 mg/kg slowly Onset: 1 min.

Peak: 5-7 min.

Duration: 2-4 hr.

Metabolized: liver

Excreted: kidney

Reduce dose by 1/3 to 1/2 when given with other CNS depressing drugs or in the debilitated.

Naloxone(Narcan)

P- Debilitated- SVT- Seizure disorders- Respiratory conditionsC- Hypersensitivity- MAO inhibitors past 14 daysS- CNS/resp. depression- Hypotension- N/V

Page 30: Pharmacology of sedative drugs (30 08-15)

Thiopental (Pentothal)

General anaesthetic agent

Initial dose:50 - 100 mgUsual maximum:3mg/kgIncremental and maximum doses are reduced to 1/3- 1/2 in the elderly.

Onset: 1- 2 min Peak: 4-8 minDuration of Action: 10 - 30 minMetabolized: liverExcreted: kidney

Reduce dose to 1/3 to 1/2when given with other CNS depressing drugs or in the inactive or debilitated.

Not recommended outside the OR.

- S- Hypotension, myocardial depression, CNS and respiratory depression, nausea, vomiting, diarrhea, laryngospasm

C- Respiratory conditionsPorphyrias

KETAMINE(Ketalar)

General anaesthetic agent

Initial dose:0.2 - 1.0 mg/kg

Usual maximum:2mg/kg.

Onset: 30 sec. IV3-4 min. IM

Duration: 5-10 min. IV12-25 min. IM

Full Recovery: 30-120 minInitial IV dose over 60 sec.(rapid administration may cause respiratory depression)

Antisecretory agent such as atropine (.01mgm/kg) or scopalamine given priorBarbituates and Ketamine should not be injected using the same syringe.

Not recommended outside the OR.

- S- Nystagmus,resp. depression, hypersalivation, laryngospasm, non- purposeful movements, emesis, HR,B/P, ICP- “Emergence reaction”- Unpleasant dreams/hallucinations(most common in females>age 10)

C- Hx CV disease or hypertension- Active pulmonary infection or disease- Head injury- Glaucoma or acute globe injury- Psychosis- Conditions with intracranial hypertension- Seizure or CNS disorders- Hx of airway instability, tracheal surgery or stenosis

Propofol (Diprivan)

General anaesthetic agentAnti-emeticAnti-convulsant

Initial dose:10 - 20mg incremental doses every 5 minutes as needed

Usual Maximum: 100mg.

Give slow IV push to avoid hypotension.

Onset: 30 sec

Duration of Action: 10 - 15 min

Reduce dose by 1/3 to 1/2when given with other CNS depressing drugs or in the inactive or debilitated.

Restricted to monitored ICU/ED patients and/or use by anesthesia personnel

- S- Respiratory depression, - HR,B/P

P- Hx CV disease or hypotension- Active pulmonary infection or disease- Concomitant use with narcotics- Hx of airway instability, tracheal surgery or stenosis

Page 31: Pharmacology of sedative drugs (30 08-15)

Reversal Agents for Drugs used for Adult and Pediatric Sedation

DRUG

ACTION&

ONSET

ADMINISTRATION GUIDELINES

(In Adults)

PEDIATRIC DOSING SPECIAL CONSIDERATIONS

PRECAUTIONS CONTRAINDICATIONS

SIDE EFFECTS

NALOXONE(Narcan)

Reversal of narcotics

Onset: 1-2 min.

0.4mg. –2mg. IV

May repeat as needed in 2-3 min. intervals PRN

0.01mg/kg every 2-3 min.

May repeat as needed.

If does not produce desired outcome a subsequent dose of 0.1mg/kg may be administered.

Alternate infusion at 0.4mg/hour

Can precipitate VT/VF in patients with CV disease or receiving potentially cardiotoxic drugs.

P - Cardiovascular disease

C- Hypersensitivity- Narcotic dependency

S- N/V, sweating- Tachycardia, hypertension- Pulmonary edema

FLUMAZENIL(Anexate)

Reversal of benzodiazepine

induced sedation

Onset: 1-2 min.

Peak effect: 6-10 min.High Risk people may be necessary to increase interval between doses to over one minute.

Initial dose:0.2mgm. IV over 15 sec.Wait 45 sec, additional 0.2mg. doses at one minute intervals until maximum of 4 additional doses have been given.

Maximum cumulative dose is 1.0 mg.Repeat above in 20 min. if neededNo more than 3 mg. in one hour.

No manufacturer published recommendations

Can precipitate seizures in those with seizures controlled by benzodiazepines, with tricyclic depression overdose & with high risk for seizures.

P - Resedation, monitor for resedation, respiratory depression for up to 120 min. Resedation least likely in low dose sedation, (eg < 10mg Versed)

C- Hypersensitivity- Tricyclic antidepressant overdose- Benzodiazepine dependency

S - Visual disturbances, diaphoresis, seizures, arrhythmias

Page 32: Pharmacology of sedative drugs (30 08-15)

BEN

ZOD

IAZEPIN

ES

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BEN

ZOD

IAZEPIN

ES• BINDING: Strongly bind to

plasma proteins• DISTRIBUTION: Highly lipid

soluble and accumulate in body fat

• t ½: MIDAZOLAM = 1.5-2.5 hrs, DIAZEPAM = 30-100 hrs

• METABOLISM: HEPATIC; hydroxylation and conjugation with glucuronic acid

• EXCRETION: Renal (urine), milk.• Freely cross placental barrier.• 1st trimester fetal abnormalities• 3rd trimester fetal dependence

and floppy-infant syndrome.

Page 35: Pharmacology of sedative drugs (30 08-15)

BEN

ZOD

IAZEPIN

ES

Page 36: Pharmacology of sedative drugs (30 08-15)

Adult SedationMidazolam (Dormicum):• A Benzodiazepine.

• Initial Dose: 1 - 2.5 mg (max. 2.5 mg).

• Maximum: 3.5 - 5 mg in 30 min.

• How to administer: Evaluate Your Patient first insert & secure IV Give The Initial Dose Slowly Wait 2 min to evaluate effects Give Incremental Dosing in order to maintain sedation level with ¼ of the initial dose DO NOT EXCEED MAX DOSE.

• Onset: 1 ½ -5 min - Peak: 10-15 min - Duration: 60-90 min.

• Recovery is dose dependent, usually 1-2 hrs.

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• Pediatric Patients Less Than 6 Months of Age No manufacturer published recommendations

• Pediatric Patients 6 Months to 5 Years of Age: 0.05 to 0.1 mg/kg

• Pediatric Patients 6 to 12 Years of Age: 0.025 to 0.05 mg/kg

Pediatric Sedation Midazolam

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• Elderly • Debilitated • Respiratory Disorders

• CNS / Resp. depression• Hypotension• Agitation• N/V• Hiccups

• Hypersensitivity• Acute narrow angle glaucoma

Page 39: Pharmacology of sedative drugs (30 08-15)

Adult Sedation

Diazepam (Valium):• A Benzodiazepine.

• Initial Dose: 2 mg (max. 2.5 mg).

• Maximum: 10-20 mg in 30 min (1/2 this dose in the elderly).

• How to administer: Evaluate Your Patient first insert & secure IV Give The Initial Dose Slowly Wait 5-10 min to evaluate effects Give Incremental Doses in order to maintain sedation level with ¼ of the initial dose DO NOT EXCEED MAX DOSE.

• Onset: 1-5 min - Peak: 20 min - Duration: 15-60 min.

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• No manufacturer published recommendations

• > 1 month of age: 0.25 mg/kg over 3 min; Can repeat in 15-30 min until total of 0.75mg/kg (MAX DOSE)

Pediatric Sedation Diazepam

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• Elderly • Debilitated • Respiratory Disorders

• CNS / Resp. depression• Hypotension• N/V• Dizziness

• Hypersensitivity• Acute narrow angle glaucoma• Psychosis

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Potency

• Midazolam > Diazepam = 4:1

• Diazepam is a more cumulative drug, it has a long half life (≈30 hrs). Midazolam t½ =1-2hrs; less cumulative.

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Adult SedationFentanyl:• A Potent Opioid.

• Initial Dose: 25-50 µg.

• Maximum: 100-250 µg in 30 min.

• How to administer: Evaluate Your Patient first insert & secure IV Give The Initial Dose Slowly Wait 5 min to evaluate effects Give Incremental Dosing in order to maintain sedation level with ¼- ½ of the initial dose DO NOT EXCEED MAX DOSE.

• Onset: 1-2 min - Peak: 3-5 min - Duration: 30-60 min.• Recovery is dose dependent, usually 1 hr.

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• No manufacturer published recommendations

• We try 0.25-1 µg/kg/dose.

Pediatric Sedation Fentanyl

Page 45: Pharmacology of sedative drugs (30 08-15)

• Elderly • Debilitated • Respiratory Disorders• Bradyarrhythmias• Head injury

• CNS / Resp. depression• Hypotension, bradycardia• N/V, pruritus, seizures• Muscle rigidity

• Hypersensitivity

Page 46: Pharmacology of sedative drugs (30 08-15)

OPIO

ID A

GEN

TS• Derivatives of opium or synthetic derivatives

resembling the natural opioid agents• Morphine and codeine are naturally occurring agents

in opium• Extensively metabolized in the liver• Excreted in Urine• Meperidine is not recommended for use beyond

48hrs from build up of metabolites and risk of convulsions

• Bind to receptors in the CNS & PNS

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Adult Sedation

Morphine:• An Opioid.

• Initial Dose: 2.5-10 mg.

• Maximum: 10 mg in 30 min.

• How to administer: Evaluate Your Patient first insert & secure IV Give The Initial Dose Slowly Wait 5 min to evaluate effects Give Incremental Dosing in order to maintain sedation level with ¼- ½ of the initial dose DO NOT EXCEED MAX DOSE.

• Onset: 1 min - Peak: 15 min - Duration: 2-4 hrs.

Page 49: Pharmacology of sedative drugs (30 08-15)

• 0.05 - 0.1 mg/kg slowly

Pediatric Sedation Morphine

Page 50: Pharmacology of sedative drugs (30 08-15)

• Elderly • Debilitated • Respiratory Disorders• Seizure disorders• Head injury

• CNS / Resp. depression• Hypotension• N/V, pruritus• Dizziness

• Hypersensitivity• Biliary colic

Page 51: Pharmacology of sedative drugs (30 08-15)

Adult Sedation

Meperidine, Pethidine (Demerol):• An Opioid.

• Initial Dose: 25-50 mg.

• Maximum: 100 mg in 30 min.

• How to administer: Evaluate Your Patient first insert & secure IV Give The Initial Dose Slowly Wait 5 min to evaluate effects Give Incremental Dosing in order to maintain sedation level with ⅓ - ½ of the initial dose DO NOT EXCEED MAX DOSE.

• Onset: 1 min - Peak: 5-7 min - Duration: 2-4 hrs.

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• 1 - 2 mg/kg slowly

Pediatric Sedation Demerol

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• Elderly • Debilitated • Respiratory Disorders• Seizure disorders• SVT

• CNS depression• Resp. depression

• Hypersensitivity• MAO inhibitors• Hypotension• N/V

Page 54: Pharmacology of sedative drugs (30 08-15)

Potency

Fentanyl > Morphine > Pethidine

Fentanyl > Morphine : 100 times

Morphine > Pethidine : 10 times

In equivalent doses ..0.1 mg/kg Morphine=

1mg/kg Pethidine=1µg/kg Fentanyl

Page 55: Pharmacology of sedative drugs (30 08-15)

Important Steps

Reversal of Sedation Drugs

1. Stop administering sedating/anesthetic agents

2. Open the airway / support ventilation

3. Support the circulation

4. Adminstre a reversal agent(s) in accordance to the given overdosage agent

5. Call for help !!

Page 56: Pharmacology of sedative drugs (30 08-15)

What’s The Most Important Part of a ….

Given “tool”?

THE CONCEPT OF RESCUE

Page 57: Pharmacology of sedative drugs (30 08-15)

Rescue from sedation means Rescue of a patient from a deeper level of sedation than intended is an intervention by a

practitioner proficient in airway management and life support measures

Adult sedation BLS and preferably ACLS

Pediatric Sedation BLS and preferably PALS

Page 58: Pharmacology of sedative drugs (30 08-15)

GOT TOO MUCH PAPERWORK??

RememberRemember, it’s a…, it’s a…

Page 59: Pharmacology of sedative drugs (30 08-15)

Maintain Continual Contact With Your Patient

Page 60: Pharmacology of sedative drugs (30 08-15)

JUST

OPEN THE AIRWAY

Page 61: Pharmacology of sedative drugs (30 08-15)

Reversal Agents for Drugs used for Adult and Pediatric Sedation

DRUG

ACTION&

ONSET

ADMINISTRATION GUIDELINES

(In Adults)

PEDIATRIC DOSING SPECIAL CONSIDERATIONS

PRECAUTIONS CONTRAINDICATIONS

SIDE EFFECTS

NALOXONE(Narcan)

Reversal of narcotics

Onset: 1-2 min.

0.4mg. –2mg. IV

(1-2 up to 100 micrograms/kg) May repeat as needed in 2-3 min. intervals PRN

0.01mg/kg every 2-3 min.

May repeat as needed.

If does not produce desired outcome a subsequent dose of 0.1mg/kg may be administered.

Alternate infusion at 0.4mg/hour

Can precipitate VT/VF in patients with CV disease or receiving potentially cardiotoxic drugs.

P - Cardiovascular disease

C- Hypersensitivity- Narcotic dependency

S- N/V, sweating- Tachycardia, hypertension- Pulmonary edema

FLUMAZENIL(Anexate)

Reversal of benzodiazepine

induced sedation

Onset: 1-2 min.

Peak effect: 6-10 min.High Risk people may be necessary to increase interval between doses to over one minute.

Initial dose:0.2mg IV over 15 sec.Wait 45 sec, additional 0.2mg. doses at one minute intervals until maximum of 4 additional doses have been given.

Maximum cumulative dose is 1.0 mg.Repeat above in 20 min. if neededNo more than 3 mg. in one hour.

No manufacturer published recommendations

Can precipitate seizures in those with seizures controlled by benzodiazepines, with tricyclic depression overdose & with high risk for seizures.

P - Resedation, monitor for resedation, respiratory depression for up to 120 min. Resedation least likely in low dose sedation, (eg < 10mg Versed)

C- Hypersensitivity- Seizure disorders- Tricyclic antidepressant overdose- Benzodiazepine dependency

S - Visual disturbances, diaphoresis, seizures, arrhythmias

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Naloxone:

1. The reversal agent for opioid agents2. The dose may need to be repeated because the

duration of action of naloxone may be shorter than that of the narcotic being reversed

3. Acute narcotic reversal may cause pain, nausea, vomiting, hypertension and CHF

4. Desired effects are alertness and adequate ventilation without discomfort; naloxone should be titrated to effect in 0.1 mg increments to avoid serious side effects

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Flumazenil:

1. Is a specific reversal agent for benzodiazepines?

2. May cause seizures in benzodiazepines dependent patients

3. Should be titrated in effect in 0.2 mg. increments over one minute

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Risk Reduction Associated with Conscious Sedation

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Causes of complicationsAssociated with Conscious Sedation Agents

• Inappropriate patient selection

• Unanticipated response

• Inappropriate monitoring of pharmacological effects

• Over-medication

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Improve Patient Selection

• Use the ASA classification

• Assess airway

• Assess neurologic, psychological, and cardiorespiratory fitness

• Follow NPO guidelines

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Prepare for Unexpected Events

• Anticipate for known abnormal reactions

• Adequate preparation of all necessary equipment

• Call for help

• Basic/Advanced life support

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Adequate Monitoring of Drug Effects

• Establish standard monitoring for ALL CASES

• Maintain continual patient contact and observation

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Prevention of Oversedation

• Use standard drug dosage and precautions (use distributed leaflets)

• Titrate dosage to response

• Allow enough time to a drug to appear

• Get reversal agents as well as other emergency drugs in reach of your hand

• Basic/Advanced life support

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Any Questions

?

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Summary

• Choose your patient carefully, learn about his/her body weight and comorbidities.

• Check and understand your monitoring and resuscitation equipment

• Use medication judiciously, remember you can’t take it out but you can always give more!

• Have reversal agents available but always remember basic resuscitation techniques.

• Be vigilant and prepare for the unexpected.

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