ESAU KIPLANGAT NGENO

HB101/G/7985/19
ANAESTHESIA

Discuss: fentanyl, morphine ,sufentanil, alfentanil, remifentanil under the following topics:
physical and chemical properties, systemic effects, dosage and techniques, uses, advantages,
disadvantages and safety measures

REMIFENTANIL
Physical and Chemical Properties

Chemical Structure: Remifentanil is a synthetic opioid analgesic belonging to the class of opioids known as the 4-anilidopiperidine derivatives.

Appearance: Typically, it is a white to off-white powder.

Solubility: Remifentanil is highly soluble in water.

Systemic Effects:

Analgesia: Remifentanil provides potent analgesia by acting as a selective μ-opioid receptor agonist.

Respiratory Depression: One of the most significant side effects, it can cause dose-dependent respiratory depression, which necessitates careful
monitoring during administration.
Cardiovascular Effects: Remifentanil may lead to bradycardia, hypotension, and alterations in cardiac output due to its effects on the cardiovascular
system.

Pharmacology

Mechanism of Action: Remifentanil binds to μ-opioid receptors in the central nervous system, inhibiting neurotransmitter release and modulating
pain perception.

Metabolism: Unlike many other opioids, remifentanil is rapidly metabolized by nonspecific tissue and plasma esterases, leading to its short duration
of action.

Half-life: Remifentanil has an ultrashort half-life, typically around 3-10 minutes, due to its rapid metabolism.

Dosage and Techniques

Infusion: Remifentanil is commonly administered via continuous intravenous infusion during surgical procedures.

Dosage: The dosage of remifentanil varies based on factors such as patient age, weight, and the nature of the procedure. It is typically adjusted to
achieve the desired level of analgesia while minimizing adverse effects.

Uses

Anesthesia: Remifentanil is frequently used as part of balanced anesthesia to provide intraoperative analgesia and supplement general anesthesia.

Procedural Sedation: It may also be utilized for procedural sedation in settings such as intensive care units or emergency departments.

Labor Analgesia: In some cases, remifentanil may be used for labor analgesia, although its short duration of action may limit its effectiveness in this
context.

Advantages

Rapid Onset: Due to its rapid metabolism, remifentanil offers a swift onset of action, making it suitable for achieving prompt analgesia.

Controlled Duration: Its short half-life allows for precise titration and rapid recovery after discontinuation.
Predictable Clearance: Remifentanil's metabolism is not influenced by hepatic or renal function, resulting in predictable clearance across a broad
range of patients.

Disadvantages:

Respiratory Depression: Its potent respiratory depressant effects necessitate vigilant monitoring and careful dose titration to prevent adverse
events.

Tolerance and Dependence: Prolonged use may lead to the development of tolerance and physical dependence, requiring cautious management
during withdrawal.

Cost: Remifentanil can be more expensive than other opioid analgesics, potentially limiting its accessibility in some healthcare settings.

Safety Measures

Continuous Monitoring: Patients receiving remifentanil should undergo continuous monitoring of vital signs, particularly respiratory rate and
oxygen saturation.

Titration: Dosage should be titrated carefully to achieve adequate analgesia while minimizing the risk of respiratory depression.

Rescue Medications: Antagonists such as naloxone should be readily available to reverse the effects of remifentanil in case of overdose or
respiratory depression.

Alfentanil

Physical and Chemical Properties

Chemical Structure: Alfentanil is a synthetic opioid analgesic belonging to the phenylpiperidine class.

Appearance: Typically, it is a white to off-white crystalline powder.

Systemic Effects

Analgesia: Alfentanil provides potent analgesia by acting as a selective μ-opioid receptor agonist.

Respiratory Depression: Similar to other opioids, Alfentanil can cause dose-dependent respiratory depression.

Cardiovascular Effects: Alfentanil may lead to bradycardia, hypotension, and alterations in cardiac output.

Pharmacology

Mechanism of Action: Alfentanil acts primarily on μ-opioid receptors in the central nervous system, inhibiting neurotransmitter release and
modulating pain perception.

Metabolism: Alfentanil undergoes hepatic metabolism primarily via cytochrome P450 enzymes.

Half-life: Alfentanil has a relatively short half-life, typically around 1-2 hours.

Dosage and Techniques

Infusion: Alfentanil is commonly administered via continuous intravenous infusion during surgical procedures.

Dosage: Dosage varies based on patient factors and the nature of the procedure, with adjustments made to achieve optimal analgesia while
minimizing adverse effects.

Uses

Anesthesia: Alfentanil is frequently used as part of balanced anesthesia to provide intraoperative analgesia and supplement general anesthesia.

Procedural Sedation: It may also be utilized for procedural sedation in settings such as intensive care units or emergency departments.

Labor Analgesia: In some cases, Alfentanil may be used for labor analgesia, although its short duration of action may limit its effectiveness.

Advantages
Rapid Onset: Alfentanil offers a rapid onset of action, making it suitable for achieving prompt analgesia.

Intermediate Duration: While shorter-acting than some opioids, Alfentanil's duration of action is longer compared to drugs like remifentanil.

Predictable Pharmacokinetics: Alfentanil's metabolism is relatively predictable, allowing for more precise dosing adjustments.

Disadvantages:

Potential for respiratory depression.

Limited use in prolonged surgical procedures.

Safety Measures:

Continuous monitoring of respiratory and hemodynamic parameters.

Dose adjustments based on patient characteristics.

FENTANYL
Physical and Chemical Properties:

Synthetic opioid, highly lipophilic, belonging to the phenylpiperidine class.

Potent and fast-acting, with a high affinity for opioid receptors.

Systemic Effects:

Rapid onset within minutes, short duration of action (30-60 minutes).

Produces profound central nervous system depression, leading to analgesia, sedation, and respiratory depression.

Pharmacology:
Potency: Extremely potent, about 50-100 times more potent than morphine.

Mechanism: Binds to mu-opioid receptors, producing potent analgesic effects.

Duration: Short-acting, leading to rapid onset and offset.

Dosage and Techniques:

Administered in micrograms, often through transdermal patches, intravenous or transmucosal routes.

Dosage carefully adjusted based on patient factors like age, weight, and comorbidities.

Uses:

Widely used for pain management, particularly in chronic conditions.

Anesthesia induction and maintenance, especially in cardiac surgeries.

Advantages:

High potency allows for smaller doses.

Effective in managing severe pain.

Disadvantages:

Risk of respiratory depression, especially in opioid-naive patients.

Potential for abuse and overdose.

Safety Measures:

Continuous monitoring of vital signs, particularly respiratory rate.

Controlled distribution due to abuse potential.

MORPHINE
Physical and Chemical Properties:

Naturally occurring alkaloid derived from the opium poppy.

Moderate lipophilicity, belonging to the phenanthrene class of opioids.

Systemic Effects:

Slow onset (15-30 minutes), extended duration of action (3-6 hours).

Induces analgesia, euphoria, sedation, and respiratory depression.

Pharmacology:

Potency: Less potent compared to fentanyl.

Mechanism: Binds to mu-opioid receptors, resulting in analgesic effects.

Duration: Intermediate duration of action.

Dosage and Techniques:

Administered in milligrams, available in various formulations including oral, intravenous, and intramuscular.

Dosage adjusted based on the severity of pain and patient response.

Uses:
Mainstay for pain relief in various medical settings.

Frequently used in palliative care and postoperative pain management.

Advantages:

Well-established efficacy and safety profile.

Versatile in different routes of administration.

Disadvantages:

Slower onset compared to synthetic opioids.

Side effects include constipation, nausea, and potential for addiction.

Safety Measures:

Monitoring for respiratory depression, particularly in opioid-naive patients.

Individualized dosing based on age, renal function, and concomitant medications.

SUFENTANIL
Physical and Chemical Properties:

A synthetic opioid, highly lipophilic, belonging to the fentanyl family.

Among the most potent opioids, with a greater analgesic effect than fentanyl.

Systemic Effects:

Rapid onset (1-2 minutes), ultra-short duration of action (10-30 minutes).

Pharmacology:

Potency: Even more potent than fentanyl, approximately 5-10 times more potent.

Mechanism: Binds to mu-opioid receptors.

Duration: Short-acting, similar to fentanyl.

Dosage and Techniques:

Administered in micrograms, predominantly through intravenous routes.

Dosage carefully titrated in anesthesia to maintain hemodynamic stability.

Uses:

Primarily used in anesthesia for major surgical procedures.

Advantages:

Exceptional potency allows for precise control of analgesia.

Rapid onset and offset contribute to quick recovery after surgery.

Disadvantages:

Increased risk of respiratory depression.

Limited use outside the operating room due to its potency.

Safety Measures:

Continuous monitoring of vital signs, especially during induction and emergence.