Pharmacology Unit 9: Analgesics

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Questions and Answers

What is the primary function of COX-1 in the body?

Vascular protection and ischemia

Inflammation and pain

Fever and kidney function

Mucosa protection, platelet aggregation, and renal blood flow (correct)

Which of the following NSAIDs is considered safe by some experts?

Celecoxib

Aspirin

Ibuprofen

Naproxen (correct)

What is the effect of NSAIDs on the cyclooxygenase pathway?

Inhibition of lipoxygenase

Stimulation of prostaglandin production

Activation of phospholipase

Inhibition of prostaglandin production (correct)

What is the role of phospholipase in the arachidonic acid pathway?

Conversion of phospholipids to arachidonic acid Signup and view all the answers

What is the primary effect of leukotrienes in the lipoxygenase pathway?

Phagocyte attraction and activation Signup and view all the answers

Which of the following NSAIDs is an oxicam?

Piroxicam Signup and view all the answers

What is the therapeutic disadvantage of some NSAIDs?

All of the above Signup and view all the answers

Why should aspirin not be given to patients with dengue fever?

Aspirin affects platelet aggregation, which is already affected in dengue fever Signup and view all the answers

What is the central molecule in the arachidonic acid pathway?

Arachidonic acid Signup and view all the answers

Which of the following is an inhibitor of the lipoxygenase pathway?

Lipoxygenase inhibitors Signup and view all the answers

What is the primary challenge in clinical medicine?

Management of pain Signup and view all the answers

What is the main difference between nociceptive and neuropathic pain?

Nociceptive pain is caused by inflammation, while neuropathic pain is caused by nerve damage Signup and view all the answers

Which of the following conditions is NOT typically associated with neuropathic pain?

Asthma Signup and view all the answers

What is the primary goal of analgesic therapy?

To manage pain and improve quality of life Signup and view all the answers

What type of pain is often described as 'phantom pain'?

Neuropathic pain Signup and view all the answers

Which of the following medications is NOT typically used to treat neuropathic pain?

NSAIDs Signup and view all the answers

What is the primary mechanism of action of opioids?

Producing morphine-like effects Signup and view all the answers

What type of pain is often treated with opioids in select patients?

Severe or chronic malignant pain Signup and view all the answers

Which of the following opioids is a natural opioid analgesic produced from somniferum papaver?

Morphine Signup and view all the answers

What is the primary function of μ (mu) receptors in the central nervous system (CNS)?

Supraspinal and spinal analgesia; sedation; inhibition of respiration Signup and view all the answers

Which of the following opioid agonists has anticholinergic effects?

Meperidine Signup and view all the answers

What is the mechanism of action of non-steroidal anti-inflammatory drugs (NSAIDs)?

Inhibit the synthesis of prostaglandins Signup and view all the answers

Which of the following opioid agonists has a longer duration of action compared to the others?

Methadone Signup and view all the answers

What is the primary function of δ (delta) receptors in the CNS?

Supraspinal and spinal analgesia; modulation of hormone and neurotransmitter release Signup and view all the answers

Which of the following opioid agonists is a partial μ agonist and κ antagonist?

Buprenorphine Signup and view all the answers

What is the primary function of κ (kappa) receptors in the CNS?

Psychotomimetic effects; slowed gastrointestinal transit Signup and view all the answers

Which of the following opioid agonists can antagonize the effects of strong agonists?

Buprenorphine Signup and view all the answers

What is the primary function of non-opioid analgesics?

Remove pain without producing morphine-like effects Signup and view all the answers

What is a characteristic of COX-2 inhibitors like Celecoxib?

Less GI irritation than aspirin Signup and view all the answers

What is a therapeutic disadvantage of NSAIDs?

They have a high potential for increasing myocardial infarctions and strokes Signup and view all the answers

What is the mechanism of action of Acetaminophen in reducing fever?

Inhibiting prostaglandin synthesis in the central nervous system Signup and view all the answers

Why does Acetaminophen have a weak anti-inflammatory effect?

It is inactivated in peripheral tissues Signup and view all the answers

What is the purpose of anesthesia in medical treatment?

To prevent pain during surgery Signup and view all the answers

What is the difference between local and regional anesthesia?

Local anesthesia is used to numb a specific area, while regional anesthesia is used to numb a larger portion of the body Signup and view all the answers

What is the stage of anesthesia where the patient is monitored for the return of consciousness?

Recovery Signup and view all the answers

What is the purpose of the maintenance stage of anesthesia?

To provide sustained anesthesia Signup and view all the answers

What is the duration of the induction stage of anesthesia?

From the administration of the anesthetic to the development of effective anesthesia Signup and view all the answers

What is the purpose of continuously monitoring vital signs during the maintenance stage of anesthesia?

To balance the amount of drug inhaled and/or infused with the depth of anesthesia Signup and view all the answers

What is the primary mechanism of action of local anesthetics?

Blocking sodium channels Signup and view all the answers

Which of the following is a characteristic of ketamine?

Induces a dissociative state Signup and view all the answers

What is the primary difference between lidocaine and bupivacaine?

Duration of action Signup and view all the answers

Which of the following is a unique feature of cocaine?

It has sympathomimetic effects Signup and view all the answers

What is the primary mechanism of action of dexmedetomidine?

Providing sedation Signup and view all the answers

Which of the following local anesthetics is used primarily for spinal anesthesia?

Tetracaine Signup and view all the answers

What is the primary effect of local anesthetics on nerve conduction?

Blockage of nerve conduction Signup and view all the answers

Which of the following is a common toxicity of lidocaine?

All of the above Signup and view all the answers

What is the primary difference between amides and esters?

Specific receptors Signup and view all the answers

Which of the following is a characteristic of benzocaine?

Used exclusively for topical anesthesia Signup and view all the answers

What is the primary mechanism of action of inhaled general anesthetics?

dose-dependent CNS depression Signup and view all the answers

Which of the following inhaled anesthetics is known for its rapid induction and quick recovery?

Halothane Signup and view all the answers

What is the primary use of opioids in anesthesia?

analgesia during and after surgery Signup and view all the answers

Which of the following IV anesthetics is a potent anesthetic but weak analgesic?

Barbiturates Signup and view all the answers

What is the advantage of desflurane over other inhaled anesthetics?

low solubility in blood, leading to rapid onset and recovery Signup and view all the answers

Which of the following IV anesthetics is commonly used for induction and/or maintenance of anesthesia?

Propofol Signup and view all the answers

What is the primary difference between intravenous and inhaled general anesthetics?

route of administration Signup and view all the answers

Which of the following benzodiazepines is commonly used in conjunction with anesthetics for sedation?

Midazolam Signup and view all the answers

What is the primary advantage of sevoflurane over other inhaled anesthetics?

low pungency and non-irritating to the airways Signup and view all the answers

Which of the following IV anesthetics lacks analgesic activity?

Etomidate Signup and view all the answers

What is the most common type of pain people experience?

Nociceptive pain Signup and view all the answers

What is the primary goal of analgesic therapy?

To manage pain Signup and view all the answers

What type of pain is often described as 'phantom pain'?

Neuropathic pain Signup and view all the answers

What type of pain is often treated with opioids in select patients?

Severe or chronic malignant or nonmalignant pain Signup and view all the answers

What is the primary difference between nociceptive and neuropathic pain?

Nociceptive pain is triggered by physical damage, while neuropathic pain is not Signup and view all the answers

What type of medications are often effective for mild to moderate arthritic pain (nociceptive pain)?

NSAIDs Signup and view all the answers

What type of pain does not develop in response to specific circumstances or outside stimuli?

Neuropathic pain Signup and view all the answers

What is the term used to describe the pain from physical damage or potential damage to the body?

Nociceptive pain Signup and view all the answers

What is the primary mechanism of action of COX-2 inhibitors like Celecoxib?

Inhibiting cyclooxygenase enzymes in the central nervous system Signup and view all the answers

What is the primary therapeutic advantage of some NSAIDs?

They cause less GI irritation than aspirin Signup and view all the answers

What is the primary function of Acetaminophen?

Reducing fever and alleviating pain Signup and view all the answers

Why does Acetaminophen have a weak anti-inflammatory effect?

It is inactivated in peripheral tissues Signup and view all the answers

What is the primary purpose of general anesthesia?

To induce unconsciousness during surgery Signup and view all the answers

What is the stage of anesthesia where the anesthetic admixture is withdrawn?

Recovery Signup and view all the answers

What is the primary purpose of the maintenance stage of anesthesia?

To monitor vital signs and response to stimuli Signup and view all the answers

What is the primary difference between local and regional anesthesia?

Local anesthesia numbs a particular area, while regional anesthesia numbs a larger portion of the body Signup and view all the answers

What is the purpose of anesthesia in medical treatment?

To prevent patients from feeling pain during surgery Signup and view all the answers

What is the stage of anesthesia where vital signs and response to stimuli are continuously monitored?

Maintenance Signup and view all the answers

What is the primary mechanism of action of inhaled general anesthetics?

They cause dose-dependent CNS depression Signup and view all the answers

Which of the following is a characteristic of sevoflurane?

It has low pungency, allowing rapid induction Signup and view all the answers

What is the primary difference between intravenous and inhaled general anesthetics?

Route of administration Signup and view all the answers

Which of the following is an example of a benzodiazepine?

Diazepam Signup and view all the answers

What is the primary mechanism of action of propofol?

It enhances the activity of GABA Signup and view all the answers

Which of the following natural opioid analgesics can be produced from somniferum papaver?

Morphine Signup and view all the answers

What type of anesthetic is ketamine classified as?

Dissociative anesthetic Signup and view all the answers

Which of the following is a characteristic of desflurane?

It provides very rapid onset and recovery Signup and view all the answers

What is the primary use of opioids in anesthesia?

To relieve pain Signup and view all the answers

What is the primary mechanism of action of local anesthetics?

Blocking sodium ion channels Signup and view all the answers

Which of the following opioid receptor subtypes is primarily responsible for supraspinal and spinal analgesia?

μ (mu) Receptors Signup and view all the answers

Which of the following is a characteristic of halothane?

It was initially favored for its rapid induction and quick recovery Signup and view all the answers

What is the main difference between lidocaine and bupivacaine?

Duration of action Signup and view all the answers

What is the primary function of morphine?

All of the above Signup and view all the answers

Which of the following local anesthetics is used primarily for topical anesthesia?

Benzocaine Signup and view all the answers

Which of the following opioid agonists has anticholinergic effects?

Meperidine Signup and view all the answers

What is the primary mechanism of action of etomidate?

It is a hypnotic agent with no analgesic activity Signup and view all the answers

What is the primary difference between barbiturates and benzodiazepines?

Their mechanism of action Signup and view all the answers

What is the primary function of non-opioid analgesics?

To remove pain but do not produce the effects of morphine or narcotic effects Signup and view all the answers

What is the unique feature of cocaine?

It has sympathomimetic effects Signup and view all the answers

Which of the following opioid agonists is a partial μ agonist and κ antagonist?

Buprenorphine Signup and view all the answers

What is the primary difference between amides and esters?

Receptor binding Signup and view all the answers

What is the primary mechanism of action of non-steroidal anti-inflammatory drugs (NSAIDs)?

Inhibit the synthesis of prostaglandins Signup and view all the answers

What is the primary effect of local anesthetics on nerve conduction?

Blocked sodium ion channels Signup and view all the answers

What is the primary toxicity of lidocaine?

All of the above Signup and view all the answers

Which of the following opioid agonists can antagonize the effects of strong agonists?

Codeine Signup and view all the answers

Which of the following local anesthetics is used primarily for spinal anesthesia?

Tetracaine Signup and view all the answers

What is the primary function of δ (delta) receptors in the CNS?

All of the above Signup and view all the answers

Which of the following opioid agonists has a longer duration of action compared to the others?

Methadone Signup and view all the answers

What is the primary mechanism of action of dexmedetomidine?

Alpha-2 adrenergic receptor agonism Signup and view all the answers

What is the primary function of COX-2 in the body?

Related to pathophysiology and adaptation such as inflammation, pain, fever, ischemia, kidney function, and vascular protection Signup and view all the answers

What is the role of cyclooxygenase in the arachidonic acid pathway?

Conversion of arachidonic acid to prostaglandins Signup and view all the answers

What is the effect of non-steroidal anti-inflammatory drugs (NSAIDs) on the cyclooxygenase pathway?

Inhibition of cyclooxygenase Signup and view all the answers

Which of the following NSAIDs is a propionic acid?

Ibuprofen Signup and view all the answers

What is the primary effect of prostaglandins in the body?

All of the above Signup and view all the answers

Which of the following is a therapeutic advantage of selected NSAIDs?

Low cost Signup and view all the answers

What is the primary function of phospholipase in the arachidonic acid pathway?

Conversion of phospholipids to arachidonic acid Signup and view all the answers

What is the primary effect of leukotrienes in the lipoxygenase pathway?

All of the above Signup and view all the answers

Which of the following is a characteristic of COX-1 inhibitors?

Inhibit COX-1 and COX-2 Signup and view all the answers

What is the primary function of corticosteroids in the arachidonic acid pathway?

Inhibit phospholipase Signup and view all the answers

Study Notes

Pain Management

Pain is a subjective, unpleasant sensation that can be acute or chronic, resulting from complex neurochemical processes in the peripheral and central nervous systems (CNS).
Nociceptive pain: pain from physical damage or potential damage to the body, e.g., from a sports injury, dental procedure, or arthritis.
Neuropathic pain: pain from a damaged or non-functional nervous system due to disease or injury, e.g., from conditions like alcoholism, shingles, or unmanaged diabetes.

Analgesics

Non-opioid analgesics, such as NSAIDs (nonsteroidal anti-inflammatory agents), are often effective for mild to moderate arthritic pain (nociceptive pain).
Opioids are used for severe or chronic malignant or nonmalignant pain, and for neuropathic pain.
Opioids can be divided into chemical classes: natural, semisynthetic, and synthetic.

Opioid Agonists

Morphine: a strong μ-receptor agonist with variable affinity for δ and κ receptors.
Effects: analgesia, relief of anxiety, sedation, slowed gastrointestinal transit.
Clinical applications: severe pain, adjunct in anesthesia, pulmonary edema, maintenance in rehabilitation programs.
Pharmacokinetics/toxicities: first-pass effect, duration 1-4 hours, toxicity includes respiratory depression, constipation, addiction liability, convulsions.

Mixed Opioid Agonist-Antagonists

Buprenorphine: a partial μ agonist, κ antagonist.
Effects: like strong agonists but can antagonize their effects, also reduces craving for alcohol.
Clinical applications: moderate pain, some maintenance rehabilitation programs.
Pharmacokinetics/toxicities: long duration of action (4-8 hours), may precipitate abstinence syndrome.

Non-Opioid Analgesics

Can remove pain but do not produce the effects of morphine or narcotic effects.
General safety: most can be bought over-the-counter (OTC).

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

Mechanism of action: inhibit the synthesis of prostaglandins.
Prostaglandins: created from arachidonic acid by the cyclooxygenase enzyme; the major mediator of pain and inflammation.

Examples of NSAIDs

Aspirin, Celecoxib, Diclofenac, Diflunisal, Etodolac, Fenoprofen, Flurbiprofen, Ibuprofen, Indomethacin, Ketorolac, Ketoprofen, Mefenamic Acid, Meloxicam, Methyl Salicylate, Nabumetone, Naproxen, Oxaprozin, Piroxicam, Salsalate, Sulindac, Tolmetin.

Acetaminophen

Inhibits prostaglandin synthesis in the CNS.
Antipyretic and analgesic properties: reduces fever and alleviates pain.
Less effect on cyclooxygenase in peripheral tissues, resulting in weak anti-inflammatory activity.

Anesthesia

A medical treatment that prevents patients from feeling pain during surgery.
Stages: induction, maintenance, and recovery.
Types: local, regional, and general anesthesia.

General Anesthesia

Intravenous general anesthetics: Barbiturates, Benzodiazepines, Dexmedetomidine, Etomidate, Ketamine, Opioids, Propofol.
Inhaled general anesthetics: Desflurane, Halothane, Isoflurane, Sevoflurane, Nitrous Oxide.

Local Anesthesia

Block nerve conduction of sensory impulses and, in higher concentrations, motor impulses from the periphery to the CNS.
Unlike general anesthetics, local anesthetics have specific receptors.
Na⁺ ion channels: Blocked to prevent transient increase in permeability of the nerve membrane to Na⁺ required for an action potential.

Examples of Local Anesthetics

Lidocaine: Amides, blocks sodium channels, slows and then blocks action potential propagation.
Bupivacaine: Amides, same mechanism of action as lidocaine, used for longer-duration procedures.
Prilocaine, Mepivacaine, Articaine, Ropivacaine, Levobupivacaine: Additional Amides.
Chloroprocaine: Esters, used for very short procedures.

Pain Management

Pain is a subjective, unpleasant sensation that can be acute or chronic, resulting from complex neurochemical processes in the peripheral and central nervous systems (CNS).
Nociceptive pain: pain from physical damage or potential damage to the body, e.g., from a sports injury, dental procedure, or arthritis.
Neuropathic pain: pain from a damaged or non-functional nervous system due to disease or injury, e.g., from conditions like alcoholism, shingles, or unmanaged diabetes.

Analgesics

Non-opioid analgesics, such as NSAIDs (nonsteroidal anti-inflammatory agents), are often effective for mild to moderate arthritic pain (nociceptive pain).
Opioids are used for severe or chronic malignant or nonmalignant pain, and for neuropathic pain.
Opioids can be divided into chemical classes: natural, semisynthetic, and synthetic.

Opioid Agonists

Morphine: a strong μ-receptor agonist with variable affinity for δ and κ receptors.
Effects: analgesia, relief of anxiety, sedation, slowed gastrointestinal transit.
Clinical applications: severe pain, adjunct in anesthesia, pulmonary edema, maintenance in rehabilitation programs.
Pharmacokinetics/toxicities: first-pass effect, duration 1-4 hours, toxicity includes respiratory depression, constipation, addiction liability, convulsions.

Mixed Opioid Agonist-Antagonists

Buprenorphine: a partial μ agonist, κ antagonist.
Effects: like strong agonists but can antagonize their effects, also reduces craving for alcohol.
Clinical applications: moderate pain, some maintenance rehabilitation programs.
Pharmacokinetics/toxicities: long duration of action (4-8 hours), may precipitate abstinence syndrome.

Non-Opioid Analgesics

Can remove pain but do not produce the effects of morphine or narcotic effects.
General safety: most can be bought over-the-counter (OTC).

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

Mechanism of action: inhibit the synthesis of prostaglandins.
Prostaglandins: created from arachidonic acid by the cyclooxygenase enzyme; the major mediator of pain and inflammation.

Examples of NSAIDs

Aspirin, Celecoxib, Diclofenac, Diflunisal, Etodolac, Fenoprofen, Flurbiprofen, Ibuprofen, Indomethacin, Ketorolac, Ketoprofen, Mefenamic Acid, Meloxicam, Methyl Salicylate, Nabumetone, Naproxen, Oxaprozin, Piroxicam, Salsalate, Sulindac, Tolmetin.

Acetaminophen

Inhibits prostaglandin synthesis in the CNS.
Antipyretic and analgesic properties: reduces fever and alleviates pain.
Less effect on cyclooxygenase in peripheral tissues, resulting in weak anti-inflammatory activity.

Anesthesia

A medical treatment that prevents patients from feeling pain during surgery.
Stages: induction, maintenance, and recovery.
Types: local, regional, and general anesthesia.

General Anesthesia

Intravenous general anesthetics: Barbiturates, Benzodiazepines, Dexmedetomidine, Etomidate, Ketamine, Opioids, Propofol.
Inhaled general anesthetics: Desflurane, Halothane, Isoflurane, Sevoflurane, Nitrous Oxide.

Local Anesthesia

Block nerve conduction of sensory impulses and, in higher concentrations, motor impulses from the periphery to the CNS.
Unlike general anesthetics, local anesthetics have specific receptors.
Na⁺ ion channels: Blocked to prevent transient increase in permeability of the nerve membrane to Na⁺ required for an action potential.

Examples of Local Anesthetics

Lidocaine: Amides, blocks sodium channels, slows and then blocks action potential propagation.
Bupivacaine: Amides, same mechanism of action as lidocaine, used for longer-duration procedures.
Prilocaine, Mepivacaine, Articaine, Ropivacaine, Levobupivacaine: Additional Amides.
Chloroprocaine: Esters, used for very short procedures.

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Description

This quiz covers the management of pain and analgesics, including the definition of pain, its types, and how to alleviate it. Learn about nociceptive and neuropathic pain and how analgesics work.