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MUSCULOSKELETAL DRUGS
MUSCULOSKELETAL DRUGS
325
Pharmacology
Professional
02/13/2012

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Cards

Term
Prednisone
Definition
Corticosteroid- inhibits phospholipase A
Asthma, Arthritis, Lupus
Term
Betamethasone
Definition
Corticosteroid- inhibits phospholipase A
Asthma, Arthritis, Lupus
Term
Dexamethasone
Definition
Corticosteroid- inhibits phospholipase A
Asthma, Arthritis, Lupus
Term
Triamcinolone
Definition
Corticosteroid- inhibits phospholipase A
Asthma, Arthritis, Lupus
Term
Dazoxiben
Definition
Thromboxane Antagonist-leaves prostacyclin synthesis intact so fewer AEs than aspirin
AE- loss of platelet aggregation- bleeding
Term
Pirmagrel
Definition
Thromboxane Antagonist-leaves prostacyclin synthesis intact so fewer AEs than aspirin
AE- loss of platelet aggregation- bleeding
Term
Ridogrel
Definition
Thromboxane Antagonist-leaves prostacyclin synthesis intact so fewer AEs than aspirin
AE- loss of platelet aggregation- bleeding
Term
Aspirin
Definition
Non-selective COX1 and COX2 inhibitor- COVALENT BOND IS PERMANENT-
Platelets become useless-
Ulcers, bleeding, asthma exacerbation, bronchospasm, angioedema
Term
Indometacin
Definition
NSAID- Inhibits COX1 more than COX2
Term
Sulindac
Definition
NSAID- Inhibits COX1 more than COX2
Term
Meclofenamate
Definition
NSAID- Inhibits COX1 and COX2 equally
Term
Ibuprofen
Definition
NSAID- Inhibits COX1 and COX2 equally
Term
Celecoxib
Definition
NSAID- Inhibits COX2 more than COX1
Term
Rofecoxib
Definition
NSAID- Inhibits COX2 more than COX1
Term
Propionic Acid NSAIDS- list
Definition
Ibuprofen, Naproxen, Ketoprofen, Flurprofen
(PROFENS)
Term
Propionic Acid NSAIDS- attributes
Definition
For pain, fever, arthritis, dysmenorrhea, gout
AE- GI hemorrhage, ulceration, perforation, nephrotoxic, stevens-johnson syndrome
Term
Cyclobenzaprine- indications
Definition
Spasmolytic for acute conditions
Term
Two drugs that reduce abnormally elevated muscle tone without paralysis
Definition
Baclofen, Dantrolene
Term
Atracurium- MOA
Definition
Neuromuscular blocker that interferes with transmission at the neuromuscular end plate- NON-CENTRALLY ACTING MUSCLE RELAXANT
Term
Pancuronium- MOA
Definition
Neuromuscular blocker that interferes with transmission at the neuromuscular end plate- NON-CENTRALLY ACTING MUSCLE RELAXANT
Term
Gallamine- MOA
Definition
Neuromuscular blocker that interferes with transmission at the neuromuscular end plate- NON-CENTRALLY ACTING MUSCLE RELAXANT
Term
Baclofen, diazepam, tizanidine- MOA
Definition
Centrally acting muscle relaxants
-spasmolytics
Term
Botox- Indication
Definition
Spasticity- centrally-acting muscle relaxant
Term
Diazepam- indication
Definition
Spasticity- centrally-acting muscle relaxant
Term
Tizanidine- Indication
Definition
Spasticity- centrally-acting muscle relaxant
Term
Baclofen- indication
Definition
Spasticity- centrally-acting muscle relaxant
Term
What is a peripherally acting drug for spasticity?
Definition
Dantrolene
Term
What is the mechanism of Baclofen?
Definition
Acts in spinal cord to suppress hyperactive reflexes involved in regulating muscle movement
-STRUCTURAL ANALOG OF GABA
-may mimic actions of GABA on spinal nerves
Term
What drug facilitates GABA mediated presynaptic inhibition?
Definition
Diazepam
Term
What drug interferes with release of excitatory neurotransmitters (GABA-B)?
Definition
Baclofen
Term
What drug acts at the level of the spinal cord to restore inhibiting tone?
Definition
Baclofen
Term
What drug is an agonist for the Alpha2 receptor that is inhibitory for glutamate in the lower motor neuron?
Definition
Tizanidine
Term
What drug reduces spasticity associated with MS, spinal cord injury, and cerebral palsy but is NOT effective in stroke and does NOT relieve the spasticity of Parkinson's disease?
Definition
Baclofen
Term
What is the effect of baclofen on flexor and extensor spasms and resistance to passive movement?
Definition
Baclofen decreases flexor and extensor spasms and suppresses resistance to passive movement
Term
When is baclofen preferred to dantrolene?
Definition
In patients whose spasticity is associated with significant muscle weakness
Term
If the default tone of the lower motor neuron is too high and there is not enough influence from the upper motor neuron, what drug reinforces the signal from the upper motor neuron that has been lost?
Definition
Baclofen
Term
Why is compliance low with Baclofen?
Definition
T1/2 is 2.5-4 hours, so patients have to take it too often
Term
Where is baclofen metabolized and excreted?
Definition
Metabolized in the liver, excreted by the kidneys
Term
What are the most common side effects of Baclofen?
Definition
CNS- depressant- dizziness, drowsiness, weakness, fatigue
GI Tract
Term
What are the contraindications of using Baclofen?
Definition
NO ALCOHOL or other CNS depressants
-potentiates the depressant action of these drugs
Term
What anxiolytic treats both spasticity and spasm?
Definition
Diazepam
Term
What is the MOA of diazepam?
Definition
It acts within the CNS by facilitating GABA-A mediated PRESYNAPTIC INHIBITION
-it mimics the actions of GABA-A at receptors in the spine AND brain
Term
What drug is preferred over dantrolene in patients whose strength is marginal, and causes sedation in most patients at therapeutic dosage?
Definition
Diazepam
Term
What is the major side effect of Dantrolene?
Definition
WEAKNESS
Term
What are the 4 drugs that interact badly with Baclofen and what is the interaction?
Definition
Alcohol
Antihistamines
CNS Depressants
MAO Inhibitors
CNS depression; risk of hepatotoxicity with combination of chloroxazone and alcohol
Term
What are the drugs that interact badly with Chlorphenesin and what is the interaction?
Definition
Tricyclic antidepressants- Increased CNS depression; risk of hepatotoxicity with combination of chloroxazone and alcohol
Term
What drug acts directly on skeletal muscle to relieve spasticity?
Definition
Dantrolene PERIPHERALLY ACTING
Term
What is the mechanism of action of dantrolene?
Definition
Blocks the ryanidine receptor-
SUPRESSES CALCIUM RELEASE FROM THE SARCOPLASMIC RETICULUM which
decreases the ability of skeletal muscle to contract
Term
What are two important therapeutic uses of Dantrolene?
Definition
Spasticity
MALIGNANT HYPERTHERMIA
Term
What causes malignant hyperthermia?
Definition
Excessive calcium release- caused by certain drugs- basically, the ryanidine receptor freaks out- muscles twitch causing HEAT
Term
What are the symptoms of malignant hyperthermia, and how is it treated?
Definition
Muscle rigidity, profound elevated temperature from massive calcium release inducing muscle contraction
TREAT WITH DANTROLENE TO BLOCK Ca RELEASE
Term
What are the adverse effects of Dantrolene?
Definition
Liver damage- test liver function before administering
BAD COMBINATION WITH ESTROGEN
Also, drowsiness, dizziness, malaise, lightheadedness, insomnia, fatigue, confusion, urinary frequency
Term
What muscle relaxant causes urinary frequency?
Definition
Dantrolene
Term
What are the drugs that Dantrolene interacts negatively with?
Definition
Estrogen (LIVER TOXIC)
CNS Depressants- sedation
Clindamycin
Verapamil
Warfarin
Clofibrate
Tolbutamine
Term
What happens if you give Dantrolene to someone on Clindamycin?
Definition
Increased neuromuscular blockade
Term
What happens if you give Dantrolene to someone on Verapamil?
Definition
Hyperkalemia and cardiac depression
Term
What muscle relaxant is also an antifungal and antibiotic?
Definition
Chlorphenesin
Term
Carisoprodol is a :
Definition
Centrally acting drug for acute local muscle spasm of the lower motor neuron
Term
Chlorzoxazone is a:
Definition
Centrally acting drug for acute local muscle spasm of the lower motor neuron
Term
What drug for acute local muscle spasm of the lower motor neuron is given for INJURY-RELATED spasms?
Definition
Cyclobenzaprine
Term
What drug for acute local muscle spasm of the lower motor neuron is given for strains and sprains?
Definition
Metaxalone
Term
What drug for acute local muscle spasm of the lower motor neuron makes for HIGH RISK IN THE ELDERLY?
Definition
Methocarbamol
Term
What muscle relaxant is a GABA transaminase inhibitor?
Definition
Vigabatrin
Term
What drug for acute local muscle spasm is contraindicated during pregnancy?
Definition
Chlorphenesin
Term
Chloroxazone is a :
Definition
Drug used for acute local muscle spasm
Term
Orphenadrine is a :
Definition
Drug used for acute local muscle spasm WITH ANTICHOLINERGIC PROPERTIES
Term
How do most drugs for acute LOCAL muscle spasm work?
Definition
They act as a sedative or at the level of the spinal cord or brainstem
Term
What drug is the prototype of the drugs for acute local muscle spasm, and is believed to have muscarinic effects?
Definition
Cyclobenzaprine
Term
When is cyclobenzaprine ineffective?
Definition
Muscle spasm due to cerebral palsy or spinal cord injury
Term
Does cyclobenzaprine have high protein binding or low?
Definition
Very High- 93%
Term
Does Baclofen have high protein binding or low?
Definition
Low- 30%
Term
Does Dantrolene have high protein binding or low?
Definition
Very High- >90%
Term
Does tizanidine have high protein binding or low?
Definition
Low, 30%
Term
When is Baclofen contraindicated?
Definition
Skeletal muscle spasms caused by rheumatoid arthritis
Term
When is Carisoprodol contraindicated?
Definition
Patients with known hypersensitivity to meprobamate
Term
When is Cyclobenzaprine contraindicated?
Definition
MI, Cardiac conduction disorders, hyperthyroidism
Term
When is dantrolene contraindicated?
Definition
Active hepatic disease, muscle spasms caused by rheumatoid arthritis, patients taking estrogen (because of liver toxicity)
Term
What is the MOA of tizanidine, and what are its side effects?
Definition
Alpha2 agonist- hypotension, drowsiness, and dry mouth
Term
When is botulinum toxin indicated?
Definition
Spasticity from cerebral palsy, cosmetic surgery
Term
What is the definition of a spasmolytic?
Definition
A drug that reduces abnormally elevated muscle tone without paralysis
Term
Describe spasms:
Definition
Sudden, violent, painful, involuntary contractions of a muscle or a group of muscles
Term
What neurons are involved with spasm?
Definition
Damage to LOWER MOTOR NEURON
Term
What NTM is released from the nerve terminal to stimulate a receptor to produce muscle contractions, and what is its receptor?
Definition
Acetylcholine, Nicotinic Receptor
Term
What is the definition of spasticity?
Definition
An increase in passive stretch resistance of a muscle or muscle group- movements are stiff and awkward
CONDITION IS PERMANENT
Term
List 7 common causes of spasticity:
Definition
Head injuries, cerebral palsy, MS, stroke, Alzheimers, Parkinsons, Upper Motor Neuron Lesions
Term
Spasticity is a condition of what neurons?
Definition
Upper Motor Neurons
Term
The spindle sends a monitoring signal to the spinal cord via what type of motor neuron?
Definition
1a
Term
The spinal cord sends a reflex signal to the muscle via what type of neuron (after receiving monitoring signal from the spindle)?
Definition
Extrafusal Efferents and Fusimotor Efferents
Term
The ventral root carries the motor signal heading in what direction?
Definition
Going OUT
Term
What kind of signal is carried by the dorsal root?
Definition
Sensory from periphery to spinal cord
Term
What type of nerve carries stretch information to the spinal cord?
Definition
Ia
Term
What is the MOA of cortisol?
Definition
Induce lipocortin to inhibit phospholipase A which ELIMINATES ALL ARACHIDONIC ACID DERIVATIVES
Term
What is the effect of corticosteroids on inflammation cells?
Definition
Redistribution of neutrophils, lymphocytes, monocytes, eosinophils, and basophils
Term
What is the effect of corticosteroids on macrophages?
Definition
A decrease in the ability of macrophages to release TNFAlpha and IL1, metalloproteinase, and plasminogen factor
Term
What do TNFAlpha and IL1 stimulate with regards to the action of corticosteroids?
Definition
They stimulate Phospholipase A- corticosteriods decrease release of TNFAlpha and IL1 from macrophages, thereby reducing the stimulation of Phospholipase A
Term
What is the effect of corticosteroids on mast cells, and on cytokines in general?
Definition
Decrease in synthesis of protaglnadins, leukotrienes, thromboxane, and histamine
Term
How do corticosteroids effect COX2 expression?
Definition
They inhibit expression of COX2
Term
Prednisone is what type of drug?
Definition
Synthetic corticosteroid
Term
Triamcinolone is what type of drug?
Definition
Synthetic corticosteroid
Term
Dextamethasone is what type of drug?
Definition
Synthetic Corticosteroid
Term
Fludrocortisone is what type of drug?
Definition
Synthetic corticosteroid
Term
Which synthetic corticosteroid interferes with the aldosterone receptor and has both cortisol AND aldosterone properties?
Definition
Fludrocortisone
Term
What are the main ways that synthetic corticosteroids are different from natural corticosteroids (cortisol)?
Definition
-difference in affinity for mineralcorticoids and glucocorticoid receptors
-different protein binding affinity; rate of elimination; metabolic products
Term
Hydrocortisone is what type of drug?
Definition
Corticosteroid
Term
Betamethasone is what type of drug?
Definition
Corticosteroid
Term
What is the effect of cortisol on insulin?
Definition
OPPOSITE OF INSULIN- physiological antagonist
Term
What synthetic corticosteroid has the highest salt and water retaining activity?
Definition
Fludrocortisone
Term
What are the joint related indications for corticosteroids?
Definition
Osteoarthritis, rheumatoid arthritis, psoriatic arthritis, bursitis, tenosynovitis
Term
What are the GI related indications for corticosteroids?
Definition
Crohn's disease; Ulcerative Colitis
Term
Under what conditions is it OK to give corticosteroid for inflammatory GI issues, and what needs to be ruled out?
Definition
Only give steroids if the issue is IDIOPATHIC- always rule out H. Pylori
Term
What mediates inflammation in Crohn's disease and is suppressed by corticosteroids?
Definition
LEUKOTRIENES
Term
What mediates inflammation in asthma and is suppressed by corticosteroids?
Definition
LEUKOTRIENES
Term
What skin condition is treated with corticosteroids?
Definition
Dermatitis
Term
What head problem is treated with corticosteroids ?(awkward question, I know)
Definition
Temporal Arteritis (Giant cell arteritis)
Term
What is the effect of corticosteroids on electrolytes (salt, potassium) and sugar?
Definition
Na+ retention
HYPOkalemia
HYPERglycemia
Glycosuria
Term
What is the effect of corticosteroids on blood pressure?
Definition
Hypertension (remember, we are retaining water)
Term
Why do corticosteroids cause hypokalemia?
Definition
Sodium is ALWAYS retained at the expense of potassium
Term
What is the effect of corticosteroids on bone?
Definition
Osteoporosis
Term
When are corticosteroids contraindicated?
Definition
Peptic Ulcers, hypertension, osteoporosis, heart failure
Term
What are some of the negative effects of long term use of NSAIDS?
Definition
Increased bleeding time
Dyspepsia
Subepithelial Damage and Hemorrhage
Gastric Mucosal Erosion
Frank Ulceration
Frank Zappa
Gastric Mucosal Necrosis
Term
What effect does long term NSAID use have on blood vessels?
Definition
Decrease blood vessel sensitivity to bradykinins and histamine
Term
What effect does long term NSAID use have on the kidneys?
Definition
Decreased GFR
Term
What is the mode of action of aspirin?
Definition
Irreversible inhibition of COX1 and COX2- inhibits Prostaglandins, Thromboxanes AND Prostacyclins
Term
What is the difference between the action of aspirin on endothelium versus platelets?
Definition
Endothelium can make new COX to replace that which is inhibited by aspirin
Platelets have no nuclei, can't make more COX, are rendered useless
Term
What is the effect of aspirin on NADPH oxidase?
Definition
Reduction- reduce neutrophils oxidative burst
Term
Inhibition of which COX leads to aspirin-triggered lipoxins?
Definition
COX2
Term
What is the clinical usefulness of low doses of aspirin?
Definition
Long term prevention of thrombosis and ischemia
Term
What conditions are prevented/reduced by aspirin?
Definition
Transient ischemic attacks, unstable angina, coronary artery thrombosis
Term
Aspirin is synergistic with what other drugs in pain management?
Definition
Synergistic with opioids- use in combo with morphine against cancer pain
Term
What is Reye Syndrome?
Definition
Severe adverse effect of aspirin in children
Term
What is the effect of aspirin in patients with asthma?
Definition
Airway hyperactivity
Term
What 6 NSAIDs can produce adverse effects in asthma patients?
Definition
Aspirin, indomethacin, naproxen, ibuprofen, mefenamate, phenylbutazone
Term
What are the clinical uses of ibuprofen?
Definition
Arthritis, anklyosing spondylitis, gout, primary dysmenorrhea
Term
What is special about Naproxen as an NSAID?
Definition
Long half life, 20 times more potent than aspirin, less severe adverse effects
Term
What NSAID directly inhibits leukocyte function?
Definition
Naproxen
Term
Indomethacin is what type of drug?
Definition
NSAID
Term
Sulindac is what type of drug?
Definition
NSAID
Term
Etodolac is what type of drug?
Definition
NSAID
Term
Diclofenac is what type of drug?
Definition
NSAID
Term
Ketorolac is what type of drug?
Definition
NSAID
Term
What is unique about the MOA of indomethacin, sulindac, etodolac, diclofenac, and ketorolac?
Definition
They decrease the availability of arachidonic acid IN ADDITION TO COX INHIBITION
-other eicosanoids are affected
Term
What NSAID is a direct inhibitor of neutrophil motility and promotes closure of patent ductus arteriosus?
Definition
Indomethacin
Term
What drug is given to CLOSE a patent ductus, and what drug is given to MAINTAIN a patent ductus?
Definition
To close: Indomethacin
To maintain: Alprostadil
Term
What drug, used for renal stone-associated pain, decreases the intracellular concentration of arachidonic acid?
Definition
Diclofenac
Term
What NSAID is given for renal stone associated pain?
Definition
Diclofenac
Term
What strong analgesic is used in post-surgical patients?
Definition
Ketorolac
Term
What is unique about the mechanism of action of mefenamate and meclofenamate?
Definition
They antagonize prostanoid receptors to various degrees, and have less anti-inflammatory activity and more adverse effects than aspirin
Term
What drug is used ONLY for primary dysmenorrhea, and antagonizes prostanoid receptors?
Definition
Mefenamate
Term
What drug is used to treat arthritis and antagonizes prostanoid receptors?
Definition
Meclofenamate
Term
Meclofenamate is used to treat:
Definition
Arthritis
Term
Mefenamate is used to treat:
Definition
Primary Dysmenorrhea
Term
Diclofenac is used to treat:
Definition
Renal stone associated pain
Term
Ketorolac is used when?
Definition
In post-surgical patients, for treating pain
Term
What drug is as efficacious as aspirin, naproxen, and ibuprofen against arthritis and is better tolerated?
Definition
Piroxicam
Term
What drug inhibits collagenase, proteoglycanase, and the oxidative burst?
Definition
Piroxicam
Term
What arthritis drug can be administered once a day?
Definition
Piroxicam
Term
Piroxicam is used to treat:
Definition
Arthritis (give once a day)
Term
What pro-drug is more selective for COX2 and causes less GI disturbance?
Definition
Nabumetone
Term
Nabumetone is more selective for :
Definition
COX2
Term
Acetaminophen, unlike aspirin, lacks what important use?
Definition
NOT ANTIINFLAMMATORY
Term
Why is acetaminophen better for children than aspirin?
Definition
Aspirin can cause Reyes syndrome
Term
What are the 2 main indications for acetaminophen?
Definition
Analgesic, antipyretic
Term
What is the toxicity risk of acetaminophen?
Definition
May cause kidney and liver damage
Term
What mediates toxicity in acetaminophen?
Definition
CYP2E1 and CYP3A4 mediate toxicity via release of N-Acetyl-benzoquinone imine
Term
Under what conditions would acetaminophen have less use and more side effects?
Definition
Some people have a faster CYP450
Term
What is the MOA of celecoxib?
Definition
COX2 selective inhibitor
Term
What are the main indications for celecoxib?
Definition
Osteoarthritis, rheumatoid arthritis, primary dysmenorrhea, familial adenomatous polyposis
Term
What NSAID is given for familial adenomatous polyposis?
Definition
Celecoxib
Term
What is the main risk with celecoxib?
Definition
Higher risk of cardiovascular toxicity- heart attack and stroke
Term
What is adalimumab?
Definition
Anti-TNF Alpha monoclonal antibody
-human IgG1
Term
What is Etanercept?
Definition
Anti-TNF Alpha monoclonal antibody
-dimeric fusion protein
Term
What is infliximab?
Definition
Anti-TNF Alpha monoclonal antibody
-human mouse chimeric
Term
What do the anti-TNF alpha monoclonal antibodies suppress?
Definition
IL-1, IL-6, and adhesion molecules involved in leukocyte migration
Term
What is the main risk of using anti-TNF alpha monoclonal antibodies?
Definition
Lymphoma
Term
What monoclonal antibody that has no effect on TNF Beta is used to treat rheumatoid arthritis?
Definition
Adalimumab
Term
Adalimumab is used to treat:
Definition
Rheumatoid arthritis
Term
What monoclonal antibody is used to treat rheumatoid arthritis and psoriatic arthritis?
Definition
Etanercept
Term
Etanercept is used to treat:
Definition
Rheumatoid arthritis and psoriatic arthritis
Term
What monoclonal antibody can be combined with methotrexate?
Definition
Etanercept
Term
What monoclonal antibody is used to treat Crohn's disease, ulcerative colitis, rheumatoid arthritis, anklyosing spondylitis, and psoriatic arthritis?
Definition
Infliximab
Term
Infliximab is used to treat:
Definition
Crohn's disease, ulcerative colitis, rheumatoid arthritis, ankylosing spondylitis, and psoriatic arthritis
Term
What mediator is found in the synovial fluid in rheumatoid arthritis and how does this affect treatment?
Definition
LEUKOTRIENES- give anti-leukotriene drugs
Term
What inflammatory mediator is primary in ankylosing spondylitis?
Definition
Leukotrienes
Term
What is the MOA of abatacept?
Definition
Blocks T-cell activation with decrease in TNF Alpha
Term
What monoclonal antibody blocks T-cell activation and decreases TNF alpha?
Definition
Abatacept
Term
Abatacept is used to treat:
Definition
Severe resistant rheumatoid arthritis
Term
What monoclonal antibody is given to treat severe resistant rheumatoid arthritis?
Definition
Abatacept
Term
What is efalizumab?
Definition
Recombinant human anti-CD11a monoclonal antibody
Term
Efalizumab is used to treat:
Definition
Adults with severe psoriasis
Term
What monoclonal antibody is used to treat severe psoriasis?
Definition
Efalizumab
Term
What is the MOA of omalizumab?
Definition
Blocks the interaction between IgE and the FcE receptor
Term
Omalizumab is used to treat:
Definition
Resistant allergic asthma in adults and adolescents
Term
What monoclonal antibody is used to treat resistant allergic asthma in adults and adolescents?
Definition
Omalizumab
Term
What is basiliximab?
Definition
Chimeric mouse-human monoclonal antibody
Term
What is daclizumab?
Definition
Humanized IgG1 monoclonal antibody
Term
Basiliximab is used to treat:
Definition
Prophylaxis of acute organ rejection
Term
Daclizumab is used to treat:
Definition
Prophylaxis of acute organ rejection
Term
What two monoclonal antibodies are given to prevent acute organ rejection?
Definition
Basiliximab and daclizumab
Term
What is the common risk with all monoclonal antibody treatments?
Definition
CANCER
Term
What is the mechanism of action of buspirone?
Definition
5HT1A agonist- non-benzodiazepine selective
Term
Buspirone is used to treat:
Definition
Anxiety
Term
What are the advantages of Buspirone in treating anxiety?
Definition
Relieves anxiety without causing sedative, hypnotic, and euphoric effects
DOES NOT AFFECT DRIVING SKILLS
Term
What are the side effects of buspirone?
Definition
Tachycardia, palpitation, nervousness, GI distress, and paresthesia
Term
Sumatriptan is a :
Definition
5HT1D/1B receptor agonist
Term
Sumatripatn is used to treat:
Definition
Acute migraine and cluster headache attacks
Term
What drug is used to treat acute migraine and cluster headaches?
Definition
Sumatriptan
Term
What are the adverse effects of sumatriptan?
Definition
Coronary artery vasospasm; contraindicated in patients with coronary artery disease
Term
What is naratriptan?
Definition
5HT Receptor agonist
Term
What is eletriptan?
Definition
5HT Receptor agonist
Term
When are naratriptan and eletriptan contraindicated?
Definition
Patients with hepatic and renal insufficiency
Term
What is cisapride?
Definition
A 5HT4 receptor agonist
Term
What is Tegaserod?
Definition
A 5HT4 receptor agonist
Term
What drug is used to treat irritable bowel syndrome with constipation?
Definition
Tegaserod
Term
Tegaserod is used to treat what?
Definition
Irritable bowel syndrome with constipation
Term
What is the mechanism of action of ondansetron?
Definition
5HT3 receptor antagonist
Term
What type of receptor is the 5HT3 receptor?
Definition
Ion Channel- FAST ACTING
Remember: all other 5HT's are G-protein coupled
Term
Ondansetron is used to treat:
Definition
(Prevention) nausea and vomiting associated with surgery and chemotherapy
Term
What class of drugs do we give to prevent nausea and vomiting associated with surgery and chemotherapy?
Definition
5HT3 antagonists, like Ondansetron
Term
Acrivastine is a:
Definition
Second Generation Antihistamine
Term
Cetirizine is a:
Definition
Second Generation Antihistamine
Term
Azelastine is a:
Definition
Second Generation Antihistamine
Term
Loratadine is a:
Definition
Second Generation Antihistamine
Term
Desloratadine is a:
Definition
Second Generation Antihistamine
Term
Levocabastine is a:
Definition
Second Generation Antihistamine
Term
Ebastine is a:
Definition
Second Generation Antihistamine
Term
Mizolastine is a:
Definition
Second Generation Antihistamine
Term
Fexofenadine is a:
Definition
Second Generation Antihistamine
Term
Diphenhydramine is a:
Definition
First Generation Antihistamine
Term
Carbinoxamine is a:
Definition
First Generation Antihistamine
Term
Clemastine is a:
Definition
First Generation Antihistamine
Term
Dimenhydrinate is a:
Definition
First Generation Antihistamine
Term
Promethiazine is a:
Definition
First Generation Antihistamine
Term
Hydroxyzine is a:
Definition
First Generation Antihistamine
Term
Cyclizine is a:
Definition
First Generation Antihistamine
Term
Meclizine is a:
Definition
First Generation Antihistamine
Term
Cyprohetadine is a:
Definition
First Generation Antihistamine
Term
Phenindamine is a:
Definition
First Generation Antihistamine
Term
Chlorpheniramine is a:
Definition
First Generation Antihistamine
Term
Brompheniramine is a:
Definition
First Generation Antihistamine
Term
Pyrilamine is a:
Definition
First Generation Antihistamine
Term
Tripelennamine is a:
Definition
First Generation Antihistamine
Term
What class of drug is cimetidine and what are common adverse effects?
Definition
H2 Blocker for stomach acid control
Can cause diarrhea, headache, fatigue, and constipation
Term
What class of drug is ranintidine and what are common adverse effects?
Definition
H2 Blocker for stomach acid control
Can cause diarrhea, headache, fatigue, and constipation
Term
What class of drug is fomotidine and what are common adverse effects?
Definition
H2 Blocker for stomach acid control
Can cause diarrhea, headache, fatigue, and constipation
Term
Cetirizine is used to treat:
Definition
Allergic rhinitis; allergic urticaria
Term
Acrivastine is used to treat:
Definition
Allergic rhinitis
Term
Loratadine is used to treat:
Definition
Allergic rhinitis and urticaria
Term
Desloratadine is used to treat:
Definition
Allergic rhinitis and urticaria
Term
Levocabastine is used to treat:
Definition
Allergic rhinitis and urticaria
Term
Ebastine is used to treat:
Definition
Allergic rhinitis and urticaria
Term
Mizolastine is used to treat:
Definition
Allergic rhinitis and urticaria
Term
Fexofenadine is used to treat:
Definition
Allergic rhinitis and urticaria
Term
What is the MOA of the first generation antihistamines?
Definition
Inverse Agonists
Term
What are some clinical indications for first generation antihistamines?
Definition
Rhinitis, conjunctivitis, urticaria, pruritus (itching), anaphylaxis, insomnia, motion sickness, Parkinsonism
Term
What are the common adverse effects of first generation antihistamines?
Definition
Sedation, dizziness, pupillary dilation, dry eyes, dry mouth, urinary retention, hesitancy
Term
What are the major contraindications for first generation antihistamines?
Definition
Narrow angle glaucoma
Peptic Ulcers
Term
Name three drugs that act on leukotrienes:
Definition
Zafirlukast, montelukast, zileuton
Term
What three drugs inhibit thromboxanes?
Definition
Dazoxiben, pirmagrel, ridogrel
Term
What serious issue can occur with inhibiting PI2?
Definition
Renal failure
Term
What effect do prostacyclins have on vasculature?
Definition
Vasodilation
Term
What is the mechanism of action of dazoxiben?
Definition
Specific antagonist of thromboxanes
Term
What is the mechanism of action of pirmagrel?
Definition
Specific antagonist of thromboxanes
Term
What is the mechanism of action of ridogrel?
Definition
Specific antagonist of thromboxanes
Term
What is the clinical application of thromboxane antagonists, and what advantage do they have?
Definition
Same as aspirin and NSAIDS- because they only inhibit thromboxanes, they leave prostacyclin synthesis intact so have less side effects
Term
What are the adverse effects of taking thromboxane antagonists?
Definition
Bleeding- loss of platelet aggregation
Term
What are 3 adverse effects of NSAID use?
Definition
Gastric irritation, nephrotoxicity, hepatotoxicity
Term
What two NSAIDs are most likely to cause GI disturbances?
Definition
Diclofenac, sulindac
Term
What is the difference between COX1 and COX2?
Definition
COX1 is the "housekeeping cocks"- it is on constitutively
COX2 is the inducible COX, which activates with inflammation
Term
Indometacin and sulindac are more selective for which COX?
Definition
COX1
Term
Meclofenamate and ibuprofen are more selective for which COX?
Definition
Equally Selective for both
Term
Celecoxib and rofecoxib are more selective for which COX?
Definition
COX2
Term
What are some adverse effects of aspirin?
Definition
GI ulcers, bleeding, asthma exacerbation, bronchospasm, and angioedema
Term
Ibuprofen, naproxen, ketoprofen, and flurprofen are given for what indications?
Definition
Pain, fever, arthritis(es), dysmenorrhea, gout
Term
What are the adverse effects of ibuprofen, naproxen, ketoprofen, and flurprofen?
Definition
GI Hemorrhage, ulceration, perforation, nephrotoxicity, and stevens-johnson syndrome
Term
Sulindac is given for:
Definition
Long term treatment of rheumatoid arthritis
Term
Etodolac is given for:
Definition
Long term treatment of rheumatoid arthritis
Term
Ketorolac is given for:
Definition
Long term treatment of rheumatoid arthritis
Term
What drug is given for closure of a patent ductus arteriosus?
Definition
Indomethacin
Term
Piroxicam is used to treat:
Definition
Rheumatoid arthritis, osteoarthritis, and PRIMARY DYSMENORRHEA
Term
What is the adverse effect of piroxicam?
Definition
GI bleeding worse than aspirin
Term
Nabumetone is given for:
Definition
Arthritis
Term
What is the mechanism of action of acetaminophen?
Definition
COX3 inhibition
Term
What are some adverse effects of acetaminophen?
Definition
Hepatotoxicity, nephrotoxicity, hypothermia
Term
What is inhibited by Zileuton?
Definition
Leukotrienes and lipoxins
Term
Zileuton is given for:
Definition
Asthma
Term
What are the side effects of zileuton?
Definition
Urticaria, abdominal discomfort, dizziness, and insomnia
Term
What two drugs ONLY inhibit leukotrienes?
Definition
Montelukast and Zafirlukast
Term
What is the difference between montelukast/zafirlukast and zileuton?
Definition
In contrast to zileuton, monet. and zafir. keep LIPOXINS around
Term
Montelukast is used to treat:
Definition
Perennial and seasonal allergic rhinitis
Term
Both montelukast and zafirlukast are used to treat:
Definition
Asthma
Term
What are the adverse effects of montelukast and zafirlukast?
Definition
GI distress, hallucination, agitation
Allergic granulomatous, angiitis, hepatitis
Term
What two cytokines can terminate pregnancy at any stage secondary to uterine contraction?
Definition
PGE2 and PGF2 alpha
Term
What drug is a synthetic PGE2?
Definition
Dinoprostone
Term
Dinoprostone is used for:
Definition
Induction of labor at term
2nd trimester abortion
Missed abortion
Benign hydatidiform mole
Term
What are the adverse effects of dinoprostone?
Definition
Prolonged vaginal bleeding and severe menstrual cramps can occur if used for menstrual regulation or early abortion
Term
What eicosanoid enhances pain transmission?
Definition
PGE
Term
What eicosanoid terminates the inflammatory effect?
Definition
Lipoxins, made by lipoxygenase
Term
What PGE1 derivative is given along with mifepristone for early abortion?
Definition
Misoprostol
Term
Misoprostol is given for:
Definition
Peptic Ulcers from NSAIDS
Early abortion (if given with mifepristone)
Term
What PGF2 analog is given for 2nd trimester abortion?
Definition
Carboprost
Term
Carboprost is a synthetic version of which eicosanoid?
Definition
PGF2alpha
Term
Carboprost is given for:
Definition
2nd trimester abortion
Resistant postpartum hemorrhage
Term
What eicosanoids are responsible for severe menstrual pain in dysmenorrhea?
Definition
PGE2 and PGF2 alpha
Term
Dysmenorrhea is easily treated with:

Why?
Definition
NSAIDS- decrease activity of COX so no production of PGE2 and PGF2 alpha
Term
What are the adverse effects of carboprost?
Definition
GI Disturbances, dystonia, pulmonary edema
Term
What drug, a PGE1 analog, is given to treat erectile dysfunction?
Definition
Alprostadil
Term
Alprostadil is given for:

How?
Definition
Erectile dysfunction (second line)

Intracavernosal injection (may cause penile pain, obviously- OUCH!)
Term
What effect does PGE have on vasculature?
Definition
VASODILATION
Term
Treprostinil and epoprostenol are synthetic versions of what eicosanoid?
What do they treat?
Definition
PGI2; pulmonary hypertension
Term
What effect do lipoxins have on vasculature?
Definition
Vasodilation
Term
What are the side effects of Alprostadil?
Definition
Apnea, bradycardia, hypotension, hyperpyrexia
Term
Alprostadil is a synthetic analog of what eicosanoid, and it is given to treat what?
Definition
PGE1- maintenance of a patent ductus arteriosus
Term
Alprostadil is contraindicated in what condition?
Definition
Sickle cell anemia
Term
Latanoprost is a stable version of what eicosanoid, given to treat what condition?
Definition
PGF2alpha; glaucoma
Term
PGF2 alpha has what effect on vasculature?
Definition
Vasoconstriction
Term
Bimatoprost, travoprost, and unoprostone are given to treat what condition?
Definition
Glaucoma secondary to decreased intraocular pressure
Term
What drugs may cause irreversible brown pigmentation of the iris and eyelashes, conjunctivitis, blurred vision, and drying of eyes?
Definition
PGF2 alpha drugs: latanoprost, bimatoprost, travoprost, and unoprostone
Term
Name 4 cells that synthesize and store histamine:
Definition
Mast Cells, Basophils, Neurons,
Enterochromaffin-like cells of the gastric mucosa
Term
What effect does histamine have on blood vessels and airways?
Definition
Dilation
Term
What causes release of histamine from granules when mast cells are injured?
Definition
Sodium Na+
Term
What autacoids are associated with arthritis?
Definition
COX2 and PGE2
Term
What autacoids are associated with asthma?
Definition
PGD2, LTB4, LTC4 and LTD4
Term
What autacoids are associated with Crohns and ulcerative colitis?
Definition
LTB4
Term
What autacoids are associated with dysmennorhea?
Definition
PGE2 and PGF2Alpha
Term
What autacoids are associated with glomerulonephritis?
Definition
LTB4
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