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Block 4 > Block 4 Drugs > Flashcards

Block 4 Drugs Flashcards

1
Q

Glaucoma

(6)

A

·Acetazolamide
·Brimonidine
·Dorzolamide
·Latanoprost
·Mannitol
·Timolol

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2
Q

Acetazolamide

A

Glaucoma

Classification: Systemic carbonic anhydrase inhibitor

Main clinical applications: Taken orally for prophylaxis and treatment of altitude sickness, no longer a primary treatment for glaucoma

  • *Pharmacodynamics: Mechanism/Sites of Action**
  • direct inhibition of carbonic anhydrase (administered orally and parenterally)
  • reduces intraocular pressure (IOP) by 50-60%; reduction in aqueous humor production due to decreased bicarbonate ion concentration in ocular fluid

Adverse Effects: Incidence and severity are dose related and usually respond to a lowering of the withdrawal of the drug.

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3
Q

Brimonidine

(same class: apraclonidine, clonidine)

A

Glaucoma

Classification: topical selective alpha2-adrenergic agonist

Main clinical applications: is indicated for the treatment of open-angle glaucoma and ocular hypertension

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • a potent, selective alpha2-agonist that is 1000-fold more selective for the alpha2- versus the alpha1-receptor
  • decresses IOP, without casuing mydriasis, by reducing aqueous humor production and increasing uveoscleral aqueous humor outflow

Adverse Effects: xerostomia (dry mouth due to a lack of saliva), hyperemia, ocular irritation, headache, blurred vision

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4
Q

Dorzolamide

A

Glaucoma

Classification: topical carbonic anhydrase inhibitor

Main clinical applications: for the treatment of glaucoma and ocular hypertension

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • highly specific inhibitor of an isoenzyme of carbonic anhydrase, CA-II, which exerts selective control of aqueous production and IOP
  • administered topically to the eye
  • decreases bicarbonate ion concentrations in ocular fluid which results in decreased aqueous humor secretion; intraocular pressure is subsequently lowered

Adverse Effects: appear to have clinically significatn biochemical or hematologic effects when administered topically to the eye

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5
Q

Latanoprost

A

Glaucoma

Classification: topical F2alpha prostaglandin agonist

Main clinical applications: used for the treatment of elevated intraocular pressure (IOP)

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • it is a prodrug (isopropyl ester) and it is administered topically to the eye. Following ocular administration, latanoprost is absorbed through the cornea where it is hydrolyzed to the acid form to become biologically active
  • increased uveoscleral outflow of aqueous humor results in reduced intraocular pressure

Adverse Effects: increased iris pigmentation (may gradually change eye color, increasing the amount of brown pigment in the iris by increasing the number of melanosomes (pigment granules) in melanocytes

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6
Q

Mannitol

A

Glaucoma

Classification: a parenteral osmotic diuretic

Main clinical applications: used to reduce intraocular pressure

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • administered intravenously; reduces intraocular pressure (same mechanism accounts for reducing cerebral edema, intracranial pressure, cerebrospinal fluid pressure)
  • systemically, mannitol elevates blood osmolality which increases the osmotic gradient between blood and tissues, thereby facilitating the flow of fluid out of tissues (including the brain and eye) and into the interstitial fluid and blood

Adverse Effects: pulmonary congestion, fluid and electrolyte imbalance, acidosis, electrolyte loss, dryness of mouth, thirst, marked diuresis, urinary retention, edema, headache, blurred vision

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7
Q

Timolol

A

Glaucoma

Classification: topical nonselective, beta-adrenergic receptor antagonist

Main clinical applications: beta blocker; ophthalmic agent for glaucoma treatment; reduction of elevated or normal intraocular pressure occurs irrespective of the presence of glaucoma

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • blocks both beta1- and beta2-adrenergic receptors; reduces intraocular pressure by reducing aqueous humor production or possibly outflow (beta receptors in the ciliary epithelium are linked to Na,K-ATPase). When beta receptor stimulation increases movement of Na+ into the aqueous humor, water is drawn in osmotically, so this transfer rate is decreased as beta receptors are blocked.

Adverse Effects: Visual acuity, pupil size, and accommodation do not appear to be affected

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8
Q

NSAIDs

(9)

A

·Aspirin
·Celecoxib
·Diclofenac
·Ibuprofen
·Indomethacin
·Ketorolac
·Naproxen
·Sulindac
·Meloxicam

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9
Q

Aspirin

(acetylsalicylic acid: ASA)

A

NSAIDs

Classification: a nonsteroidal antiinflammatory drug (NSAID)

Main clinical applications: used for its analgesic, antiinflammatory, antipyretic, and antithrombotic effects

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • inhibits cyclooxygenase (COX) by irreversibly inhibiting COX through acetylation of a specific serine moiety (aspirin is about 170-times more potent in inhibiting COX-1 than COX-2)
  • its metabolite, salicylic acid, can inhibit prostaglandin synthesis at the site of inflammation, in vivo, and produces the majority of classic NSAID effects
  • does not suppress leukotriene synthesis by lipoxygenase pathways
  • *Adverse Effects:**
  • gastrointestinal effects are more common: nausea, vomiting, dyspepsia, epigastric discomfort, heartburn, stomach pains, gastrointestinal ulceration (6% to 31%), gastric erosions, gastric erythema, duodenal ulcers
  • acts on renal tubule; low to moderate doses may inhibit uric acid secretion
  • bleeding is associated with aspirin; hemorrhage may occur at virtually any site
  • hyperthermia, hearing loss, tinnitus: early warning signs of salicylate toxicity
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10
Q

Celecoxib

A

NSAIDs

  • *Classification:** - A nonsteroidal antiinflammatory drug (NSAID)
  • selective COX-2 inhibitor
  • *Main clinical applications: **
  • analgesic activity: is effective in cases where inflammation has caused sensitivity of pain receptors (hyperalgesia)
  • anti-inflammatory activity is due to decreased synthesis via inhibition of COX-2
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • a selective inhibitor of cyclooxygenase-2 (COX-2)
  • comparable efficacy to other NSAIDs (e.g., naproxen and diclofenac) in rheumatoid arthritis and osteoarthritis
  • due to its selective COX-2 inhibitory activity, celecoxib does not inhibit platelet aggregation as seen with aspirin or other non-selective NSAIDs; it will inhibit the production of PGI2 but not of thromboxane A2, which is produced by COX-1
  • *Adverse Effects:**
  • all NSAIDs including celecoxib cause an increased risk of serious gastrointestinal adverse effects including bleeding, ulceration, and perforation of the stomach or intestines
  • may cause an increased risk of serious cardiovascula thrombotic events, myocardial infarction, and stroke
  • risk for adverse effects may increase with duration of use
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11
Q

Diclofenac

A

NSAIDs

Classification: a nonsteroidal antiinflammatory drug (NSAID)

Main clinical applications: nonselective COX inhibitor; it is well absorbed following i.m. injection and has a rapid onset of action

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • competitively inhibits both cyclooxygenase (COX) isoenzymes, COX-1 and COX-2, by blocking arachidonate binding; results in analgesic, antipyretic, and anti-inflammatory pharmacologic effects
  • has preferential inhibitory activity for COX-2 when tested ex-vivo
  • *Adverse Effects:**
  • a low incidence of side effects; the range of effects similar to other NSAIDs
  • concern about hepatotoxicity
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12
Q

Ibuprofen

(Advil, Motrin, Nuprin)

A

NSAIDs

Classification: a nonsteroidal antiinflammatory drug (NSAID)

Main clinical applications: for mild to moderate pain

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • nonselective COX inhibitor
  • indicated for the treatment of rheumatoid arthritis, osteoarthritis, and dysmenorrhea; used for its antipyretic effects, and for the alleviation of mild to moderate pain

Adverse Effects: GI effects considered less than those for ASA; otherwise, adverse effects similar for all NSAIDs

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13
Q

Indomethacin

A

NSAIDs

Classification: a nonsteroidal antiinflammatory drug (NSAID)

  • *Main clinical applications: **
  • a potent NSAID drug with many serious side effects and should not be considered an analgesic for minor aches and pains or fever; more potent than aspirin, but is not a better analgesic
  • for anti-inflammatory and analgesic effects in the symptomatic treatment of active stages of moderate to severe rheumatoid arthritis (including acute flares of chronic disease), osteoarthritis, and ankylosing spondylitis
  • among the drugs of choice for relieving the pain, fever, redness, swelling, and tenderness of acute gouty arthritis
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • nonselective COX inhibitor
  • indomethacin is administered orally, rectally, or intravenously
  • absorption from the gut is rapid and complete. Following administration of regular release capsules, bioavailability is about 100%, with 90% of the drug absorbed within 4 hours

Adverse Effects: as for other NSAIDs; can cause serious gastrointestinal events including inflammation, bleeding, ulceration, and perforation of the esophagus, stomach, small intestine, or large intestine, which can be fatal. These serious adverse events can occur at any time, with or without warning symptoms

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14
Q

Ketorolac

A

NSAIDs

Classification: a nonsteroidal antiinflammatory drug (NSAID)

Main clinical applications: the onset and efficacy of analgesia after systemic administration are similar to morphine, but ketorolac causes less drowsiness, nausea, and vomiting
Post-marketing studies have not found IM ketorolac to be superior to oral ibuprofen for the treatment of acute musculoskeletal pain. Can be administered intraveously.

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • nonselective COX inhibitor
  • administered orally, parenterally, or as an ophthalmic solution. Parenteral and oral dosages produce similar pharmacokinetic profiles. Absorption is rapid and complete; bioavailability is 100% after oral, IV, or IM administration
  • in comparision to other NSAIDs, ketorolac has been associated an increased incidence of GI effects and has dosing restrictions to limit these effects

Adverse Effects: unlike other NSAIDs, ketorolac should only be used for up to 5 consecutive days

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15
Q

Naproxen

(Aleve, Naprosyn)

A

NSAIDs

Classification: a nonsteroidal antiinflammatory drug (NSAID)

Main clinical applications: applications similar to other NSAIDs; is usually better tolerated than aspirin or indomethacin

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • nonselective COX inhibitor
  • elimination half life is 12-17h which is longer than the effective duration of ibuprofen 4-8h (2h half life)

Adverse Effects: similar to other NSAIDs; gi effects may be less than aspirin

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16
Q

Sulindac

A

NSAIDs

Classification: a nonsteroidal antiinflammatory drug (NSAID)

  • *Main clinical applications:**
  • used for osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, bursitis/tendonitis, acute gouty arthritis
  • sulindac and celecoxib are the only NSAIDs that appear to be effective for the regression of colorectal polyps in patients with familial adenomatous polyposis

Pharmacodynamics: Mechanisms/Sites of Action - considered a non-selective NSAID

  • *Adverse Effects:** - cardiovascular events [U.S. Boxed Warning]: NSAIDs are associated with an increased risk of adverse cardiovascular events
  • gastrointestinal event [U.S. Boxed Warning]: NSAIDs may increase risk of gastrointestinal irritation, ulceration, bleeding, and perforation
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17
Q

Meloxicam

A

NSAIDs

Classification: NSAID

Main clinical applications: used to treat arthritis; it reduces pain, swelling, and stiffness of the joints (particularly, the pain caused by the inflammation of osteoarthritis), fever; and as an analgesic, especially where there is an inflammatory component

Pharmacodynamics: Mechanisms/Sites of Action - COX-1 and COX-2 inhibitor; (frequently described in the literature as a selective COX-2 inhibitor but it is considerably less selective for the COX-2 versus COX-1 isoenzyme as compared with celecoxib)

Adverse Effects: gastrointestinal toxicity and bleeding, tinnitus, headache, rash

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18
Q

Acetaminophen

A

NSAIDs

Classification: non-opioid analgesic (not an NSAID)

  • *Main clinical applications:**
  • analgesic and antipyretic activity similar to aspirin; no significant anti-inflammatory activity
  • analgesic of choice for the treatment of episodic pain in patients with underlying renal disease
  • may be preferred in elderly patients with osteoarthritis over NSAIDs due to fewer GI and renal side effects
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • does not effectively inhibit cyclooxygenase in peripheral tissues in the presence of inflammation
  • no effects on platelet function

Adverse Effects: excess of dosing may lead to dose-dependent hepatotoxicity

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19
Q

Opioids

(17)

A

·Buprenorphine
·Codeine
·Hydropmorphone
·Dextromethorphan
·Diphenoxylate
·Fentanyl
·Hydrocodone
·Loperamide
·Meperidine
·Methadone
·Morphine
·Naloxone
·Naltrexone
·Oxycodone
·Pentazocine
·Propoxyphene
·Tramadol

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20
Q

Buprenorphine

A

Opioids

Classification: analgesic - a u-receptor opioid partial agonist (also referred to as a mixed opiate agonist/antagonist)

  • *Main clinical applications:**
  • can be used for the relief of moderate to severe pain
  • sublingual administration used for the treatment of opioid dependence
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • as a u-receptor partial agonist, exhibits a ceiling to its pharmacological effects
  • very slowly dissociates from the u-receptor, which likely accounts for its longer duration of action than morphine, the unpredictability of its reversal of opioid antagonists, and its low level of manifested physical dependence

Adverse Effects: similar to those of other opioids (nausea and vomiting, drowsiness, dizziness, headache, itch, dry mouth)

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21
Q

Codeine

A

Opioids

Classification: analgesic - moderate u-receptor opioid agonist

  • *Main clinical applications:**
  • used as a single agent, and in combination with acetaminophen, ASA, or other products for mild to moderate pain control
  • good oral bioavailability

Pharmacodynamics: Mechanisms/Sites of Action - analgesic activity of codeine is primarily due to its ~10-15% conversion to morphine; morphine is the active drug

Adverse Effects: constipation, nausea, itching, vomiting, drowsiness, dry mouth, urinary retention

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22
Q

Hydromorphone

A

Opioids

Classification: analgesic - moderate to strong u-receptor opioid agonist (more potent than morphine)

Main clinical applications: for moderate to moderate-to-severe pain; low incidence of typical opioid side effects

Pharmacodynamics: Mechanisms/Sites of Action - similar to morphine

Adverse Effects: constipation, nausea and vomiting, histamine reactions (itching (pruritis), hives (urticaria), sneezing, exacerbation of asthma), mental confusion, sedation, biliary spasm, miosis, respiratory depression, truncal rigidity

23
Q

Dextromethorphan

A

Opioids

Classification: an oral, nonprescription drug used as an antitussive

  • *Main clinical applications:** - commonly used ingredient in many cough and cold preparations
  • drug is useful in treating chronic, nonproductive cough, but it has no expectorant acitvity
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • this d-isomer opioid lacks significant opioid activity except for cough suppression
  • sites in the brain have been identified where dextromethorphan binds with high affinity
  • this drug also has NMDA antagonist properties

Adverse Effects: On May 20, 2005, the FDA made a public announcement regarding dextromethorphan (DXM) and new trends in the abuse of this drug. The ingestion of pure dextromethorphan in powdered form and in excessive dose can cause death as well as other serious adverse events such as brain damage, seizure, loss of consciousness, and irregular heart beat. When ingested at recommended dosage levels for intended purposes, dextromethorphan is generally regarded as a safe and effective cough suppressant

24
Q

Diphenoxylate

A

Opioids

Classification: antidiarrheal; an opioid agonist used for the treatment of diarrhea

Main clinical applications: indicated for the control and relief of acute, nonspecific diarrhea as well as chronic diarrhea associated with inflammatory bowel disease

Pharmacodynamics: Mechanisms/Sites of Action - inhibits GI motility and slows excess GI propulsion; it does not exhibit analgesic or opiate-like effects

Adverse Effects: atropine is added to the diphenoxylate to prevent possible drug abuse; thus, high doses of the formulation can lead to antimuscarinic effects

25
Q

Fentanyl

A

Opioids

Classification: analgesic - strong agonist at u- and k-opioid receptors

  • *Main clinical applications:** - 100 ug dose of fentanyl is approximately equipotent to 10 mg of morphine (80-100x more potent than morphine)
  • fentanyl has a longer duration (4-7 hrs) of action and half-life than morphine (2-3 hrs)
  • administered parenterally, and via transmucosal or transdermal routes

Pharmacodynamics: Mechanisms/Sites of Action - similar to those of morphine, although fentanyl is much more lipophilic as compared to morphine and has a more rapid onset of action

  • *Adverse Effects:** - morphine-like adverse effects
  • following iv administration, chest wall rigidity may occur
26
Q

Hydrocodone

A

Opioids

Classification: Analgesic - moderate u-receptor opioid agonist

  • *Main clinical applications:** - is used to treat moderate to moderately-severe pain and is available combined with acetaminophen, ibuprofen or aspirin as tablets, capsules and liquid preparations; also used as an antitussive
  • hydrocodone + acetaminophen: Vicodin

Pharmacodynamics: Mechanisms/Sites of Action - moderate agonist activity at opiate receptors within the central nervous system

Adverse Effects: similar to those of other opioid analgesics; since it is often formulated with acetominophen, excessive dosing can result in liver toxicity due to acetaminophen metabolism to toxic intermediates

27
Q

Loperamide

A

Opioids

Classification: antidiarrheal; an opioid agonist used for the treatment of diarrhea

Main clinical applications: indicated for the control and relief of acute, nonspecific diarrhea as well as chronic diarrhea associated with inflammatory bowel disease

Pharmacodynamics: Mechanisms/Sites of Action - interferes with peristalsis by a direct action on the circular and longitudinal muslces of the intestinal wall to slow motility; it does not exhibit analgesic or opiate-like effects, even at high doses; no apparent tolerance to the antidiarrheal effect and no physical dependence

Adverse Effects: minor: constipation, dizziness

28
Q

Meperidine

A

Opioids

Classification: analgesic - moderate-strong u-receptor opioid agonist

Main clinical applications: for relief of moderate to severe acute pain

Pharmacodynamics: Mechanisms/Sites of Action - primarily an opioid receptor agonist

  • *Adverse Effects:**
  • Recommended only for use in very brief courses for patients who are healthy and/or have problems with other opioid agonists; not recommended for the treatment of chronic pain because of the risk of seizures with repetitive dosing and its short duration of action
  • Meperidine is metabolized to normeperidine, a compound that at high concentrations is capable of inducing seizures
  • Contraindicated with MAO inhibitors (can result in serotonin syndrome: restlessness, hyperthermia, tremor, seizures, coma)
29
Q

Methadone

A

Opioids

Classification: analgesic - strong u-receptor opioid agonist

  • *Main clinical applications:** - analgesic properties similar to morphine but with better oral bioavailability
  • most frequently used agent in medically supervised opiate withdrawal and maintenance programs
  • *Pharmacodynamics:** Mechanisms/Sites of Action - similar to morphine
  • may be administered orally or parenterally; long half life (t1/2 = 24-36h), but duration of effective analgesia is ~8h
  • also used for suppression of withdrawal symptoms from opioids

Adverse Effects: similar to morphine

30
Q

Morphine

A

Opioids

Classification: analgesic - a strong u-receptor opioid agonist

Main clinical applications: used for the relief of moderate to severe acute and chronic pain, for preoperative sedation, and as a supplement to anesthesia; administered parenterally, intrathecally, epidurally, rectally, and orally (oral bioavailability ~20-40% due to extensive first pass metabolism)

Pharmacodynamics: Mechanisms/Sites of Action - the metabolite, morphine 6-glucuronide (~10% of total dose), has significant analgesic activity and contributes to morphine’s activity, particularly with chronic administration.

Adverse Effects: constipation, nausea and vomiting, histamine reactions (itching (pruritis), hives (urticaria), sneezing, exacerbation of asthma), mental confusion, sedation, biliary spasm, miosis, respiratory depression, truncal rigidity

31
Q

Naloxone

A

Opioids

Classification: opioid receptor antagonist (affinity: u> k, g)

Main clinical applications: used to reverse the clinical effects of opioid analgesics

  • *Pharmacodynamics: Mechanisms/Sites of Action** - essentially a pure antagonist with little or no agonist activity; half-life only 1-1.5h
  • repeat doses may be required when long-acting opioids are involved
  • antagonizes both the toxic and clinical effects of opioids (respiratory depression, hypotension, and sedation are reversed but so is analgesia)
  • administered intravenously, intramuscularly, or subcutaneously
  • Note: ineffective orally due to extensie first pass metabolism

Adverse Effects: produces no physical or psychological dependence and will not worsen respiratory depression if administered for non-opioid overdose

32
Q

Naltrexone

A

Opioids

Classification: opioid receptor antagonist (affinity: u>k, g)

  • *Main Clinical Applications**: - used to reverse the clinical effects of opioid analgesics
  • Beneficial in patients who take the drug as part of a comprehensive occupational rehabilitative program or other compliance-enhancing program for opiate dependece or addiction
  • *Pharmacodynamics: Mechanism/Sites of Action** - at usual opioid concentrations, naltrexone’s greater affinity for the receptor prevents the binding of the opioid agonist to the receptor
  • pharmacodynamic properties similar to naloxone except it has better oral bioavailability and a much longer duration of action than naloxone
  • Naloxone t1/2 1-1.5h vs. naltroxene t1/2 4h (Naltrexone has an active metabolite: t1/2 13h)

Adverse Effects - nausea (10%), headache (7%), dizziness (4%), nervousness (4%), fatigue (4%), insomnia (3%), vomiting (3%)

33
Q

Oxycodone

(Oxycontin)

A

Opioid

Classification: Analgesic - moderate to strong u-receptor opioid agonist

Main clinical applications: used to control moderate to severe pain, including cancer pain, postoperative, postextractional, postpartum pain and non-pain syndromes (e.g., restless leg and Tourette syndromes)

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • analgesia effects similar to morphine
  • oxycodone can be combined with acetaminophen: Percocet
  • oxycodone can be combined wiith aspirin: Percodan
  • *Adverse Effects:**
  • reported to be as effective as morphine in relieving pain when given in equianalgesic doses and to cause less nausea and vomiting
34
Q

Pentazocine

A

Opioid

Classification: analgesic - mixed opioid partial antagonist/agonist

  • *Main clinical applications: **
  • used to treat moderate to severe pain
  • one-sixth to one-third as potent as morphine
  • at therapeutic doses, has less respiratory depression than pure opiate agonists
  • not commonly used in clinical practice due to the occurrence of dysphoric reactions and its relatively short duration of action
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • a partial u agonist and k agonist
  • effects similar to morphine-like agonists
  • *Adverse Effects:** - sedation
  • ceiling effect for respiratory depression
  • has weaker effects on smooth muscle
  • constipation and biliary colic rare
  • nausea, vomiting, and constipation are also less with pentazocine than with morphine
  • can precipitate withdrawal in individuals physically dependent on morphine-like drugs
35
Q

Propoxyphene (Darvon)

Nov. 19, 2010 withdrawn from US market

A

Opioids

Classification: weak agonist at u-opioid receptors within the central nervous system

Main clinical applications: - for mild pain; use of propoxyphene has declined due to the availablility of more effective agents (used in combination with aspirin)

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • propoxyphene is as effective or less effective than 30-60mg of codeine or 600mg of aspirin
  • the only recognized use of propoxyphene is for the treatment of mild-to-moderate pain; aspirin is probably more effective
  • sometimes used when overconcerned about addictive potential of codeine
  • *Adverse Effects:**
  • high doses of propoxyphene are limited by side effects (serious heart rhythm abnormalities)
36
Q

Tramadol (Ultram)

A

Opioid

Classification: weak opioid agonist at u-receptors (but not an opiate derivative)

  • *Main clinical applications:** - has been shown to be effective as an adjuvant to NSAID therapy in patients with osteoarthritis who experience breakthrough pain
  • treatment of postoperative pain indicates that tramadol is equivalent in analgesic relief to codeine but is less potent than acetaminophen
  • the lack of significant cardiac effects and no association with peptic ulcer disease make tramadol an alternative in some patients who may not tolerate NSAIDs

Pharmacodynamics: Mechanisms/Sites of Action - unqiue dual mechanism of pain relief: a mu-opioid receptor agonist and a weak inhibitor of norepinephrine and serotonin reuptake in the CNS which results in inhibition of pain transmission from the spinal cord to the brain

  • *Adverse Effects:**
  • effects similar to other opiate agonists (including dizziness, somnolence, nausea, constipation, dry mouth, sweating, and pruritis)
37
Q

Local Anesthetics

(6)

A

·Benzocaine

·Cocaine

·Lidocaine
·Bupivacaine
·Ropivacaine
·EMLA

38
Q

Benzocaine

A

Local anesthetics

Classification: ester type local anesthetic

  • *Main clinical applications:** - short acting (15-20 min), topical pain reliever (OTC ointment)
  • used for topical anesthesia in a wide variety of clinical situations including mucous membrane anesthesia prior to endoscopic examination or instrumentation, gag reflex suppression, and anorectal disorders and various pain syndromes
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • blockade of voltage-dependent Na+ channels; nerve impulse generation and propagation are blocked, resulting in a reversible loss of sensation
  • *Adverse Effects:**
  • Allergic reactions can occur with benzocaine because of sensitivity to the PABA metabolite
  • Can cause of methemoglobinemia (aka met-Hb, a disorder characterized by the presence of a higher than normal level of methemoglobin in the blood. Methemoglobin is a form of hemoglobin that does not bind oxygen. Because of this concern, in 2006, the Veterans Health Administration decided to stop using benzocaine sprays in procedures that require tube insertion in the larynx or pharynx or in minor surgical procedures performed in these locations; other benzocaine products and benzocaine sprays applied to exterior skin are still allowable.)
39
Q

Cocaine

A

Local anesthesics

Classification: ester type local anesthetic

Main clinical applications: used only for topical anesthesia and vasoconstriction for surgery of the nose, throat, and oral cavity

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • blockade of voltage-dependent Na+ channels; nerve impulse generation and propagation are blocked, resulting in a reversible loss of sensation
  • produces vasoconstriction (due to blockade of NE reuptake - increasing NE at sites of adrenergic innervation of blood vessels)
  • *Adverse Effects:**
  • seldom occur in the medical field; those that do may be rapid, unexpected, and severe. Other good alternatives for anesthesia are available, and many surgeons have ceased using cocaine because of its unpredictable effects and the risk of having such a highly addictive drug in the office. Toxicity is associated with increased adrenergic effects in the CNS, cardiovascular system, and respiratory system.
40
Q

Lidocaine

A

Local anesthetics

Classification: amide type local anesthetic

Main clinical applications: for all types of local anesthesia requiring moderate duration of effect (1-2h)

Pharmacodynamics: Mechanisms/Sites of Action - blockade of voltage-dependent Na+ channels; nerve impulse generation and propagation are blocked, resulting in a reversible loss of sensation

Adverse Effects: Uncommon; effects related to systemic absorption - nausea, drowsiness, mental/mood changes, ringing in the ears, dizziness, vision changes, tremors, numbness, headache; allergic reactions unlikely

41
Q

Bupivacaine

(Marcain)

A

Local Anesthetic

Classification: amide type local anesthetic

  • *Main clinical applications: **
  • indicated for the production of local or regional anesthesia or analgesia for surgery, for oral surgery procedures, for diagnostic and therapeutic procedures, and for obstetrical procedures
  • has longer duration of action than lidocaine (6-8 vs 1-2 for lidocaine)
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • blockade of voltage-dependent Na+ channels; nerve impulse generation and propagation are blocked, resulting in reversible loss of sensation

Adverse Effects: relative to other local anesthetics, bupivacaine can be markedly cardiotoxic. However, adverse drug reactions (ADRs) are rare when administered correctly. Mostly ADRs relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia. Systemic exposure to excessive bupivacaine mainly results in CNS and cardiovascular effects.

42
Q

Ropivacaine

A

Local Anesthetics

Classification: amide local anesthetic

  • *Main clinical applications:**
  • long acting local anesthetic (2-6h: varies with administration route)
  • less cardiotoxic that bupivacaine indicated for various conditions: epidural, intra-articular, major and minor nerve block and infiltration anesthesia, postoperative and labor pain management
  • slightly less potent than bupivacaine
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • blockade of voltage-dependent Na+ channels; nerve impulse generation and propagation are blocked, resulting in reversible loss of sensation
  • *Adverse Effects:**
  • uncommon; more related to administration technique and inadvertent systemic exposure
43
Q

EMLA

A

Local Anesthetic

Classification: topical anesthetic

Main clinical applications: to anesthetize the normal, intact skin prior to painful procedures, such as injections and other medical procedures

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • Eutectic mixture of local anesthetics (EMLA) cream which contains lidocaine (2.5%) and prilocaine (2.5%); (Eutectic refers to the mixing of two solids that remains as a liquid at room temperature)
  • *Adverse Effects:**
  • contraindicated in patients with a known history of sensitivity to local anesthetics of the amide type or to any other component of the product
  • skin at the site of treatment may develop erythema or edema
44
Q

Adjuvant Analgesics

(5)

A

·Topiramate
·Amitripyline
·Gabapentin
·Pregabalin
·Capsaicin

45
Q

Topiramate

A

Adjuvant Analgesic

Classification: oral anticonvulsant; neuropathic pain medication

  • *Main clinical applications:**
  • seizures associated with epilepsy; neuropathic pain conditions
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • modulates voltage-gated sodium ion channels, potentiates GABA inhibition, blocks excitatory glutamate neurotransmission, modulates voltage-gated Ca2+ channels
  • *Adverse Effects:**
  • somnolence, nausea, and numbness; weight loss
46
Q

Amitripyline

A

Adjuvant Analgesic

Classification: tricyclic antidepressant; neuropathic pain medication

  • *Main clinical applications:**
  • depression; a range of neuropathic pain conditions (e.g. postherpetic neuralgia, as well as diabetic neuropathy). (Note: the drug is not used to treat both conditions simultaneously)
  • *Pharmacodynamics: Mechansims/Sites of Action**
  • NE and 5HT reuptake inhibitor at presynaptic nerve endings; increases neurotransmitter concentration in the synapse; also, has sodium channel blocker activity and NMDA antagonist activity
  • *Adverse Effects:**
  • anticholinergic effects (blurred vision, constipation, dry mouth, sedation, tachycardia, urinary retention); can lead to delirium in elderly patients
47
Q

Gabapentin

A

Adjuvant Analgesic

Classification: oral anticonvulsant; neuropathic pain medication

  • *Main clinical applications:**
  • control of seizures associated with epilepsy
  • reduces pain and improves some quality-of-life measures in patients with a wide range of neuropathic pain syndromes, e.g. painful diabetic neuropathy, postherpetic neuralgia (PHN) - the burning, stabbing pain or aches that may last for months or years after an attack of shingles
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • efficacy not related to modulation of GABA system
  • binds to a particular subunit of the volate activated Ca2+ channel thereby reducing Ca2+ current
  • possesses high lipid solubility, is not metabolized by the liver, has no protein binding, and is devoid of the usual drug interactions (e.g. enzyme induction); and is excreted intact in the urine
  • *Adverse Effects:**
  • dizziness and sedation
48
Q

Pregabalin

A

Adjuvant Analgesic

Classification: oral anticonvulsant; neuropathic pain medication

  • *Main clinical applications: **
  • adjunt therapy for partial seizures
  • effective at treating chronic pain in disorders such as fibromyalgia and spinal cord injury
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • like gabapentin, pregabalin binds to the voltage-dependent Ca2+ channel
  • pregabalin is more potent, absorbed faster, and has greater bioavailability than gabapentin
  • *Adverse Effects**
  • dizziness and sedation
49
Q

Capsaicin

A

Adjuvant Analgesic

Classification: topical analgesic

  • *Main clinical applications: **
  • treat minor aches and pains of muscles/joints (e.g. arthritis, backache, sprains); also used the treat nerve pain
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • the active, pungent component of chili peppers; binds to the thermal nociceptors, resulting in sensation of heat. Multiple applications deplete substance P from sensory neurons, resulting in nociceptor desensitization
  • *Adverse Effects:**
  • dermatologic: ithching, stinging sensation, erythema; transient burning on application usually diminishes with repeated use
  • low patient compliance remains a significant issue due to pain upon initial application
50
Q

Skeletal Muscle Relaxants

(4)

A

·Baclofen
·Carisoprodol
·Cyclobenzaprine
·Tizanidine

51
Q

Baclofen

A

Skeletal Muscle Relaxant

Classification: skeletal muscle relaxant; spasmolytic drug

  • *Main clinical applications:**
  • used to treat spasticity and improve mobility in patients with multiple sclerosis and other spinal cord lesions
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • is a central-acting, oral skeletal muscle relaxant without direct effect on skeletal muscle
  • an agonist for the GABA B receptors (GABA B receptors are linked via G proteins to K+ channels; their activation hypopolarizes the neuron
  • *Adverse Effects:**
  • most common adverse effect of oral or intrathecal baclofen is drowsiness (63%); nausea/vomiting (4-12%), constipation (2-6%); muscular weakness and hypotonia are dose-related effects of baclofen
  • abrupt discontinuation of baclofen may result in withdrawal syndrome associated with increase spasticity, hallucinations, and seizures; baclofen therapy should be withdrawn slowly
52
Q

Carisoprodol

(Soma)

A

Skeletal Muscle Relaxant

Classification: skeletal muscle relaxant

  • *Main clinical applications: **
  • less frequently used due to the availability of newer agents
  • CNS mechanisms related to agonistic effects on the GABA A receptor, and not to a direct effect on skeletal muscle
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • is a central-acting, oral skeletal muscle relaxant without direct effect on skeletal muscle
  • *Adverse Effects:**
  • drowsiness and dizziness, which may require dosage reduction; other negative CNS effects
53
Q

Cyclobenzaprine

A

Skeletal Muscle Relaxant

Classification: skeletal muscle relaxant

  • *Main clinical applications: **
  • used for the relief of muscle spasm associated with acute, painful musculoskeletal conditions
  • ineffective in treating muscle spasm due to cerebral palsy or spinal cord injury (structurally related to the TCA, amitripytline, but not used as an antidepressant)
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • relieves muscle spasms through a central action, possibly at the brain stem level, with no direct action on the neuromuscular junction or the muscle involved. It is not a peripheral neuromuscular blocker.

Adverse Effects:
CNS depression and/or anticholinergic effects (drowsiness, xerostomia, and dizziness)

54
Q

Tizanidine

A

Skeletal Muscle Relaxant

Classification: a centrally-acting, selective alpha2-adrenergic agonist

  • *Main clinical applications: **
  • skeletal muscle relaxant used to treat the spasms, cramping, and tightness of muscles caused by multpile sclerosis, back pain, or certain injuries to the spine
  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • a central-acting alpha2-adrenergic agonist which acts at presynaptic receptors. It is structurally and pharmacologically related to clonidine, but has only 2-10% of clonidine’s antihypertensive potency. The antispasmodic activity of tizanidine results from agonism at central pre-synaptic alpha2-receptors. The response to agonism at these receptors is a decrease in the release of excitatory amino acids which in turn leads to inhibition of spinal motor neurons.
  • *Adverse Effects:**
  • asthenia (defined as weakness, fatigue and/or tiredness), sedation or drowsiness, xerostomia (dry mouth), increased spasm or tone, dizziness
  • dose-related hypotension occurred relatively frequently in patients treated with single oral doses

Block 4 (5 decks)

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