Pharm Test 1

Front 1

Diphenhydramine

Back 1

1st Generation Anti-Histamine ; 8 hrs
Therapeutic Use: Tx of H1-mediated allergic response (possible local anesthetic?)
Important Side Effects: anti-cholinergic like effects, +++ Sedation; ++antimedic; +++anticholinergic***
aka benedryl
Important Interactions: Paradoxical Stimulation in Children
antihistamine; 1st gen

Front 2

Dimenhydrinate

Back 2

8 hrs; high sedation, med antimedic; high anticholinergic
antihistamine; 1st gen

Front 3

Hydroxyzine

Back 3

to active metab cetirizine-high sed, med antimedic; high anticholinergic; has an active metab cetirizine; +++sedation
antihistamine; 1st gen

Front 4

Meclizine

Back 4

12 hrs; antiemetic high; med anticholinergic; less sedating than others so used for motion sickness or vertigo
antihistamine; 1st gen

Front 5

Chlorpheneramine

Back 5

1st Generation Anti-Histamine; less sedating than the others;
Therapeutic Use: Tx of H1-mediated allergic response to pollen, mold, spores, and other environmental
Important Side Effects: Anti-cholinergic like effects, ++ Sedation; no antimedic, ; high anticholinergic
Important Interactions: Paradoxical stimulation in children
anti-histmaine; 1st gen

Front 6

Promethazine

Back 6

D2 Antagonist – Phenothiazine antipsychotic
Therapeutic Use: used as an Anti-emetic (possible anesthetic)
Important Side Effects: Hyperprolactinemia and EPS
Important Interactions: Synergistic w/ CNS depressants
12 hrs DOA; high sedative; high antiemetic; **high anticholinergic
antihistamine; 1st gen

Front 7

how to treat anticholinergic overdose?

Back 7

physostigmine (cholinesterase inhibitor) cross BBB

Front 8

Anticholinergic effects

Back 8

Anticholinergic- dry mouth, blurred vision, tachy, urinary retention, andothe ratropine-like side effects.

Front 9

1st Generation (Older)

Back 9

1) Diphenhydramine (BENADRYL)
2) Chlorpheniramine (CHLOR-TRIMETON)
3) Pyrilamine (NISAVAL)
4) Clemastine (TAVIST)
5) Hydroxyzine (ATARAX)
6) Brompheniramine (DIMATANE)
7) Promethazine (PHENERGAN)

Front 10

2nd gen drugs

Back 10

1) Fexofenadine (ALLEGRA)
2) Loratadine (CLARITIN & ALAVERT):  Desloratadine (CLARINEX)
3) Cetirizine (ZYRTEC)
4) Desloratadine (CLARINEX)
5) Terfenadine (SELDANE): pulled from the market due to risk of PVC’s
6) Astemizole (HISMANAL): pulled from the market due to risk of PVC’s

Front 11

2nd generation H1 Rc antagonists

Back 11

do not cross BBB sig; preferred for allergies and better when given before exposure to allergen than after. Also should take regularly through allergy season; NO antiemetic activity

Front 12

2 drug pulled from marked and why

Back 12

Terfenadine; astemizole-->variety of compounds ( pulled from market) for long QT interval

Front 13

what is terfenadine's active drug?

Back 13

fexofenadine

Front 14

Fexofenadine

Back 14

2nd Generation Anti-Histamine (Terfenadine is metabolized to form Fexofenadine)
Therapeutic Use: Tx of H1-mediated allergic responses
Important Side Effects: Some anti-cholinergic effects, + sedation.
Important Interactions: few
12 hrs DOa; very low sedative; no antiemetic; very low anticholinergic

Front 15

Cetirizine

Back 15

2nd Generation Anti-Histamine (Hydroxyzine is metabolized to form Cetirizine)
Therapeutic Use: Tx of H1-mediated allergic response
Important Side Effects: some anti-cholinergic effects, + sedation
Important Interactions: synergistic effects w/ CNS depressants
24 hr DOA; low sed-more likely to cause than any other 2nd gens; no antiemetic; low anticholinergic

Front 16

Loratadine

Back 16

2nd Generation Anti-Histamine; prodrug
Therapeutic Use: Tx of H1-mediated allergic response
Important Side Effects: some anti-cholinergic effects, + sedation
Important Interactions: few
24 hr DOA; very low sedative; none antiemetic; very low anticholinergic

Front 17

Azelastine

Back 17

Nasal Anti-Histamine; more potent than sodium cormoglycate or theophylline
Therapeutic Use: Allergic Rhinitis
Important Side Effects: Drowsiness and Sedation (headache, dry mouth, weight gain)
important Interactions: few
12 hr DOA; low sedative; non antiemetic; low anticholinergic; HL 22 hrs; P450 metab; active metab is desmethylazelastine

Front 18

Buspirone

Back 18

- Class: 5HT-1A selective partial agonist
- Therapeutic Use: anxiolytic (for anxiety) and depression
- Important Side Effects: chest pain, dizziness and headache – possible REM disturbances
- Important Interactions: May increase Haloperidol plasma levels

Front 19

Sumatriptan

Back 19

Class: 5HT-1B/D selective Agonist (autoreceptors on the nerve terminals; agonist act dec release of neuropeptides.
Therapeutic Use: used for Acute Migraine attacks (useful in reversing migraines and cluster headaches)
-constriction of intracrainial bv esp AV anastomoses. Migrained due to dilation of these AV anastomoses and shunting blood away from capillary beds and producing cerebral ischemia and hypoxia; inhibit release of por-inflammatory VD neuropeptides form nerve terminals ending in the cerebrale perivascular space.
**work to prevent 2nd phase of migraines, the rebound VD effect
Important Side Effects: Coronary Vasospasm
Important Interactions: synergistic interaction w/ Ergots

Front 20

zolmitriptan

Back 20

Class: 5HT-1B/D selective Agonist
like sumatirptan
used for acute migraine attacks

Front 21

naratriptan

Back 21

Class: 5HT-1B/D selective Agonist like sumatriptan

used for acute migraine attacks

Front 22

rizatriptan

Back 22

Class: 5HT-1B/D selective Agonist like sumatriptan
used for acute migraine attacks

Front 23

Tegaserod

Back 23

only for crisis only w/ FDA approval
5HT-4 partial agonist
- Therapeutic Use: GI prokinetic agent (used in constipation and IBD) esp in women w/ IBS. Recent withdrawn due to inc risk of MI or stroke
- Important Side Effects: Mild
- Important Interactions: Few

Front 24

Methylsergide

Back 24

(anti-migraine)
5HT-2 Antagonist
- Therapeutic Use: Migraine Prophylaxis and diarrhea in carcinoid tumors
- Important Side Effects: Peripheral ischemia and chest pain, dizziness and insomnia

Front 25

Cyproheptadine

Back 25

(anti-diarrheal)
- Class: 5HT-2 selective antagonist; anti-H1 also; liquid and tablets
- -antiperistaltic in carcinoid crisis; DOC for urticaria (hives); pruritus ALSO use to counteract sexual dysfunction of 5-HT reuptake inhibitors eg fluoxetine (Prozac)
- Indications: Post-gastrectomy dumping syndrome, anti-peristaltic in carcinoid crisis, DOC for uticaria (hives), pruritis, and is also used to counteract sexual dysfunction of SSRI’s such as Fluoxetine.

Front 26

Ketanserin

Back 26

: (anti-hypertension)
- Class: 5HT-2 antagonist on sm (also an alpha-1 blocker)
- Indicated for HTN and Vasospasm (Raynaud’s disease)
- Anti-hypertensive effects may be mediated by blockade of alpha-1 adrenoceptors and/or 5HT-2 Rc on smooth muscle

Front 27

Clozapine

Back 27

: (anti-psychotic)
- Class: 5HT-2 selective Antagonist (and DA non-selective antagonist)
- Therapeutic Use: Tx of Psychosis (anti-psychotic, treats the negative symptoms of Schizophrenia) atypical antipsychotic w/ less adverse effects than traditional antipsychotic agents but agranulocytosis can occur
- Important Side Effects: Agranulocytosis
- Important Interactions: Additive effects w/ anti-cholinergics and potentiation of hypotensive effects.

Front 28

5HT-2 antagonists and Dopamine D2 antagonists

Back 28

1) Risperidone
2) Ziprasidone
3) Quetiapine
Dual action atypical anti-psychotic treats negative symptoms of Schizophrenia w/ low incidence of EPS side effects with low doses; at high doses you see EPS side effects;
not clozapine

Front 29

Ondansetron

Back 29

- Class: 5HT-3 antagonist (blocks 5HT-3 Rcs in CTZ (area postrema) and vagal afferents in GI)
- Therapeutic Use: treatment of N/V (chemotherapy induced); GI disorders
- Important Side Effects: headaches
- Important Interactions: metabolized by P450, may be effected by Cimetadine or Phenobarbital.

Front 30

Granisetron

Back 30

and dolasetron
- Class: 5HT-3 Antagonist (blocks 5HT-3 Rcs in CTZ (area postrema) and vagal afferents in GI)
- Therapeutic Use: Tx of nausea and vomiting (chemotherapy induced) ; GI disorders
- Important Side Effects: headaches
- Important Interactions: metabolized by P450, may be effected by Cimetadine or Phenobarbital.

Front 31

Fluoxetine

Back 31

SSRI ; MC class
- Therapeutic Use: depression, OCD, PMDD, panic disorder , bulimia nervosa
- Suicidal tendancies inc when people take the drug who are severely depressed b/c they gain motivation to kill themselves
- Important Side Effects: Hotflashes and heart palpitations, agitation, insomnia and decreased libido
- Important Interactions: Inhibit metabolism of carbamazepine and hydantoins. Potentiate effects of MAO-I.

Front 32

Sertraline

Back 32

indicated for major depression, panic disorder, OCD, PTSD, and PMDD

Front 33

Mirtazapine

Back 33

1st agent in a new class; antag at presynaptic (alpha) 2 adrenergic inhibitory autoreceptors and heretoreceptors leads to an inc in central nonadrenergic and serotoneric activity; a potent antag of H1 Rc (sedative)
- Class: Increases NE/5HT release and blocks 5HT-2/3 receptors
- Therapeutic Use: treatment of depression
- Important Side Effects: agranulocytosis, hypotension (alpha-1 antagonist), agitation and abnormal thought patterns.
- Important Interactions: additive effects w/ CNS depressants. MAO-I may precipitate hypertensive crisis.
SSRI MC class

Front 34

Sibutramine

Back 34

removed from market
- Class: Block uptake of 5HT / DA and NE (blocks there re-uptake)
- Therapeutic Use: used in Tx of obesity (anorectic and appetite suppression)
- Important Side Effects: increased CV response, headache and agitation, dry mouth, and vomiting
- Important Interactions: additive effects w/ MAO-I. With other 5HT agonists could cause “serotonin syndrome”
SSRI MC class

Front 35

Alprostadil

Back 35

(PGE1)- impotency, to maintain ductus arteriosus
eicosanoid

Front 36

Misoprostol

Back 36

Misoprostol (PGE1 analog)- gastric protection (cytoprotection) also as abortifacient when used with RU486 (mifepristone)
eicosanoid

Front 37

Dinoprostone

Back 37

(PGE2)- abortifacient, labor induction, cervical ripening
eicosanoid

Front 38

Carboprost

Back 38

(PGF2a analog)- post-partum bleeding, abortifacient
eicosanoid

Front 39

Epoprostenol

Back 39

(PGI2)- primary pulmonary hypertension
eicosanoid

Front 40

Treprostinil

Back 40

(PGI2 analog)- primary pulmonary hypertension
eicosanoid

Front 41

Beraprost

Back 41

(PGI2 analog)- primary pulmonary hypertension
eicosanoid

Front 42

Latanoprost

Back 42

(PGF2a analog) – glaucoma
eicosanoid

Front 43

Travoprost

Back 43

(PGF2a analog) – glaucoma; eicosanoid

Front 44

Unoprostone

Back 44

(PGF2a analog) – glaucoma
eicosanoid

Front 45

Bimatoprost

Back 45

(prostamide) - glaucoma; eicosanoid

Front 46

Dinoprostone

Back 46

contraction of uterine mm; uses PGE2; oxytocic act inc uterine contractions; NATURAL
- Class: Prostaglandin analog, “Abortifiacient”, Pregnancy Category “C”
- Therapeutic Use: vaginal insert Cervical ripening or termination of pregnancy from weeks 12-20 (suppository to evacuate uterine contents); non-malig trophoblastic disease (hydatiform mole)
- Important Side Effect: Bradycardia/syncope, abnormal uterine contraction, bronchospasm, headaches/ flushing, blurred vision. ; N/V; PYRESIS AND DIARRHEA impt!!; hypotension
- Important Interactions: Augments the action of Oxytocin agents
eicosanoid
dose w/ vaginal suppository w/ 20mg highinto vagina; additional 20mg inserted at 3-5 h until abortion is complete; max dosage 240 mg or cont use for 48hr

Front 47

Carboprost tromethamine

Back 47

Class: Analog of PGF2a; against FP receptors; -contraction of uterine sm; oxytocic activity; IM to control bleeding
- Therapeutic Use: Controls postpartum bleeding when resistant to ergonovine; abortifacient
- Important Side Effect: vasospasm, potential increase in BP; flushing, diarrhea, vominting, alt bp, blurred vision, resp distress
- Important Interactions: Diarrhea
eicosanoid

FETAL HEART BRADYCARDIA AND DECERATION, ABNL CONTRACTION, n/V????

Front 48

Alprostadil

Back 48

Class: PGE1 agonist; injectable, pellet, and cream
- Therapeutic Use: VD; Maintain PDA until surgery and treatment of ED (erectile dysfunction into cavernosa of penis)
- Important Side Effect: Bradycardia, hypotension, CHF, seizures, diarrhea, penile pain, priapism, flushing, diarrhea, headache and fever (mostly replaced by sildenafil drugs for ED); apnea w/ 10% neonates
- Important Interactions: none
eicosanoid

Front 49

Epoprostenol

Back 49

Analog of PGI-2 (prostacyclin); act on IP receptors to dilate pulmonary blood vessels and inc pulmonary BF; VD; inhibit plt agg via IP Rc
- Therapeutic Use: long term IV treatment of pulmonary arterial HTN.
- Important SE: Headaches, dizziness, diarrhea, mylagia, flushing and tachycardia, hypotension; flulike symptoms
- Important Interactions: increased risk of bleeding w/ anti-coagulants
eicosanoid

Front 50

Remodulin

Back 50

Prostacyclin approved for continuous infusion in 1o Pulmonary HTN.

eicosanoids

Front 51

Beraprost

Back 51

in phase 3 clinical trials, but is chemically stable oral form of Prostacyclin for early-stage Pulmonary HTN.
eicosanoids

Front 52

Misoprostol

Back 52

PGE1 analogue for against EP Rc; PGEs needed for mucus layer secretion; NSAIDs inhibit PG production; so replacement therapy; gastric cytoprotection (inhib gastric secretion and inc bicarb secretion); oral
- Class: Prostaglandin analog, “Abortifacient”, Pregnancy Category “X” in combo w/ mifepristone
- Therapeutic Use: Prevent PUD in NSAID users and Rx of ulcers unresponsive to H2 antagonists. Gastric and duodenal ulcers induced by NSAIDs
- Important Side Effect: headache, diarrhea, cramps and uterine contractions (CONTRAINDICATED in pregnant women b/c it can stim premature labor)
eicosanoids

Front 53

Latanoprost

Back 53

eyedrops
- Class: analog of PGF2a (agonist); inc aqueous humor outflow via uveoscleral pathway
- Therapeutic Use: Reduction of IOP in open-angle glaucoma and ocular HTN
- Important Side Effect: Increased melanin = increased brown color in iris; alter eye color
- Important Interactions: few if administered properly – effects restricted to the eye.
eicosanoids

Front 54

Bimatoprost

Back 54

- Class: Analog of PGF2a is a prostamide w/ occurlar hypotensive activity once a day dosing (better compliance) and greater efficacy; lower IOP by inc the outflow of aqueous humour through the trabecular network and uveoscleral routes
- Therapeutic Use: Reduction of IOP in open-angle glaucoma and ocular HTN
- Important Side Effect: Increased melanin = increased brown color in iris
- Important Interactions: few if administered properly – effects restricted to eye
eicosanoids

Front 55

Travoprost

Back 55

- Class: Analog of PGF2a (agonist)
- Therapeutic Use: Reduction of IOP in open-angle glaucoma and ocular HTN
- Important Side Effect: Increased melanin = increased brown color in iris
- Important Interactions: few if administered properly
eicosanoids

Front 56

Unoprostone

Back 56

- Class: Analog of PGF2a
- Therapeutic Use: Reduction of IOP in open-angle glaucoma and ocular HTN
- Important Side Effect: Increased melanin = increased brown color in iris
- Important Interactions: few if administered properly
eicosanoids

Front 57

Montelukcast

Back 57

Class: Leukotriene Cys LT1-antagonist ; antiinflammatory
- Therapeutic Use: Asthma (1 x day) ; blocks all but B4 b/c diff Rc; prevnets inflammation edema BC and formation of thick/viscous mucus--inhibits both early and late phases of VC
- Important Side Effect: well tolerated, may cause diarrhea, laryngitis, otitis, sinusitis, and nausea
- Important Interactions: avoid in NSAID-sensitive patients. Chewable tablets contain Phenylalanine.
alt for long term; may enhance B2 agonists
Leukotriene Antagonists; eicosanoids

Front 58

Zafirlukast

Back 58

Leukotriene Cys LT1-antagonist
- Therapeutic Use: Asthma (2x day) blocks actionsof LTC4,D4, E4 but not B4 (BCT1 Rc); prevents inflammation edema,BC, and formation of thick/viscous mucus- inhibits both early and late phases of constriction
- Important Side Effect: Same as Montelukast, plus rash and/or neuropathy similar to CHURG-STRAUSS, poss liver failure
-Important Interactions: Increases Warfarin effects, erythromycin and theophylline decrease Zafirlukast [], Aspirin increases [] of Zafirlukast. (this this b/c it inhibits CYP 2C9 and 3A4)
Leukotriene Antagonists; eicosanoids
anti-inflammatory agents; alt for long term use in asthma; may enhance B2 agonsits

Front 59

Zileuton

Back 59

5-Lipoxygenase inhibitor – inhibit leukotrienes synthesis; antiinflammatory agent, LT synthesis inhibitor; 4x/day; alt for long term; may enhance B2 agonists; blocks ALL LT B, D, E, C!!!
-Therapeutic Use: Asthma prophylaxis mild to moderate (not approved for but may be beneficial in RA and UC); poss more effective w/ severe
-Important Side Effect: well tolerated, may cause headaches, may elevate hepatic enzyme levels, drowsiness, dyspepsia (rapidly metabolized by glucuronidaiton)
- Important Interactions: Zileuton increases the plasma [] of Propranolol, Theophylline, and Warfarin.
Leukotriene Antagonists; eicosanoids inhibiton of CYP-1A2 and 3A4

Front 60

Ambrisentan

Back 60

much higher affinity for ETa Rc- inhib endothelin converting enzyme (ECEi); use for pulmonary art HTN likely a powerful teratogen NOT for females unless on hormonal birth control
endothelin

Front 61

Bosentan

Back 61

- Class: Nonselective blocks both ETA – ETB antagonist; oral
- Therapeutic Use: Pulmonary HTN
- Important Side Effect: Headache, nasopharyngitis, flushing, potentially serious liver damage; inc serum aminotransferase levels, so must do liver function tests monthly; major birth defects if pregnant and OCT
- Important Interactions: Interactions w/ any drugs metabolized by CYP2D9 and CYP3A4. Inhibited by oral contraceptives, cyclosporine A, glyburide, category X during pregnancy
endothelins

Front 62

Codeine

Back 62

- Class: various – weak agonist at opioid receptors – converted to morphine
- Therapeutic Use: cough suppressant
- Important Side Effect: sedation, dizziness and drowsiness. May cause N/V and constipation. High doses – opioid OD
- Important Interaction: converted to morphine by 2D6, inhibitors of 2D6 will prevent conversion to morphine
centrally acting, anti-tussives OPIOID

Front 63

Dextromethorphan

Back 63

- Class: Non-analgesic – non-addictive (?) D-isomer of Codeine
- Therapeutic Use: cough suppressant
- Important Side Effect: occasional mild drowsiness and GI upset. High doses resemble opioid toxicity
- Important Interaction: MAO inhibitors (hypotension). Inhibitors of 2D6 may increase [Dextromethorphan].
OPOID, anti-tussive; OTC b/c no high
DM

Front 64

Guaifenesin

Back 64

- Class: unknown, but increases production and flow of less viscous mucus.
- Therapeutic Use: Expectorant
- Important Side Effect: occasional nausea and vomit in high dose.
- Important Interaction: none

Front 65

hydrocodone

Back 65

can be used in resp conditions; an opioid; anti-tussive

Front 66

Beclomethasone

Back 66

orally and nasally inhaled
Inhaled glucocorticoid agonist
Therapeutic Use: inhaled – ASTHMA + ALLERGIES, intranasal (not >3 wks) – congestion; prophylactic and acute (only adverse effect if it was systemic)
-use in children w/ severe asthma but poss suppression ofthe adrenal-pituitary axis, so effect is minimal but might delay the growth but they catch up
- Important Side Effect: Candida albicans (thrush), hoarseness, dry mouth. High doses decrease HPA. IN ELDERLY MC COMPLAINT IS BURNING THROAT (DRINK SOMETHING)
- Important Interaction: none
Anti-Inflammatory agents: Glucocorticoids (decrease inflammation, edema, histamine release) Do not stop treatment abruptly
TAKES SEVERAL WEEKS TO TAKE EFFECT

Front 67

Triamcinolone

Back 67

: (orally and nasally (not greater than 3 wks) inhaled)
- Class: Inhaled glucocorticoid agonist
- Therapeutic Use: ASTHMA + ALLERGIES ; prophylactic and acute
- Important Side Effect: Candida albicans (thrush), hoarseness, dry mouth. High doses decrease HPA. N ELDERLY MC COMPLAINT IS BURNING THROAT (DRINK SOMETHING)
-use in children w/ severe asthma but poss suppression ofthe adrenal-pituitary axis, so effect is minimal but might delay the growth but they catch up
- Important Interaction: none (should not be used for more than a few weeks)
Anti-Inflammatory agents: Glucocorticoids (decrease inflammation, edema, histamine release) Do not stop treatment abruptly
TAKES SEVERAL WEEKS TO TAKE EFFECT

Front 68

Fluticasone

Back 68

- Class: Inhaled glucocorticoid agonist
- Therapeutic Use: ASTHMA + ALLERGIES; prophylactic and acute
- Important Side Effect: Candida albicans (thrush), hoarseness, dry mouth. High doses decrease HPA. N ELDERLY MC COMPLAINT IS BURNING THROAT (DRINK SOMETHING)
-use in children w/ severe asthma but poss suppression ofthe adrenal-pituitary axis, so effect is minimal but might delay the growth but they catch up
- Important Interaction: none
Anti-Inflammatory agents: Glucocorticoids (decrease inflammation, edema, histamine release) DO NOT STOP ABRUPTLY
TAKES SEVERAL WEEKS TO TAKE EFFECT

Front 69

glucocorticoids in general

Back 69

Anti-Inflammatory agents: (decrease inflammation, edema, histamine release) Do not stop treatment abruptly

Front 70

leukotriene antagonists in general

Back 70

tx only asthma; dec cAMP and inc Ca via Gq and Gi; recruit WBC, inc mucus, inc vasc perm, inc collagen, inc sm prolif, and contraciotn=inflammed airway

Front 71

Cromolyn

Back 71

- Class: mast cell membrane stabilizer (inhibits release of histamine)
- Therapeutic Use: asthma, allergic rhinitis (prophylactic only)
- Important Side Effect: ophthmalic – stinging or burning, oral – headache or diarrhea.
- Important Interaction: none (younger patients respond better, takes 4-6 weeks for therapeutic levels to be reached)

Front 72

Lodoxamide

Back 72

- Class: Mast cell membrane stabilizer in ophthalmic solution for ocular allergies (inhibits release of histamine)
- Therapeutic Use: vernal keratitis and vernal conjunctivitis
- Important Side Effect: slight stinging/burning but usually well tolerated
- Important Interaction: none

Front 73

Nedocromil

Back 73

- Class: Inhaled mast cell membrane stabilizer (inhibits release of histamine)
- Therapeutic Use: asthma
- Important Side Effect: bronchospasm, bad taste, headache
- Important Interaction: none

Front 74

mast cell stabilizers in general

Back 74

prevent degranulation; poss by blocking Ca influx; not systemic; lower oral bioavailability; few SE

Front 75

Theophylline

Back 75

Methylxanthine-related to caffiene (inhibits PDE and Ca influx and adenosine recpt) (bronchodilator) (inhibits PDE, increased cAMP, a second messenger)
- Therapeutic Use: asthma, obstructive lung disorders and apnea (inhibits mucus secretion, decreases histamine release); COPD
- Important Side Effect: no antidote for overdose; GI distress (pain, N/V and CNS/CV stimulation)
-***some cardiac stimulation tachy
- Important Interaction: Cimetidine inhibits CYP-1A2, Macrolide antibiotics inhibit clearance – other drugs may also inhibit clearance. smoke increases metabolism
phosphodiesterase inhibitor (bronchodilator)

Front 76

Ipratropium

Back 76

- Class: Peripheral muscarinic antagonist (cholinergic antagonist)
- Therapeutic Use: COPD> allergies; Emphysema, Bronchitis **NOT FOR ASTHMA
- Important Side Effect: Nasal dryness and dry mouth
- Important Interaction: none (may have synergistic effects w/ B2-agonists)

muscarinic antagonists (bronchodilater)
same as tiaproium

Front 77

tiatropium

Back 77

Class: Peripheral muscarinic antagonist (cholinergic antagonist)
- Therapeutic Use: COPD, Emphysema, Bronchitis (not asthma)
- Important Side Effect: Nasal dryness and dry mouth
- Important Interaction: none (may have synergistic effects w/ B2-agonists)
same as ipratropium

Front 78

1) Albuterol

Back 78

- Class: selective B2 Receptor Agonist; bronchodilators
- Therapeutic Use: “escape” inhaler used in acute asthma attacks
- Important Side Effect: Possible Cardiac Stimulation
- Important Interaction: beta-blockers may antagonize the effects.
less cardiac effects; fast acting

Front 79

2) Pirbuterol

Back 79

- Class: Selective Beta-2 Rc Agonist; bronchodilators
- Therapeutic Use: “escape” inhaler used in acute asthma attacks
- Important Side Effect: possible cardiac stimulation
- Important Interaction: beta-blockers may antagonize the effects
less cardiac effects; fast acting

Front 80

3) Salmeterol

Back 80

- Class: Selective Beta-2 Rc agonist; bronchodilators
- Therapeutic Use: slower/longer acting – nocturnal asthma and exercise-induced asthma (inhibits late-phase allergen-induced bronchoconstriction after short acting beta-2 agonists wear off)
- Important Side Effect: possible cardiac stimulation
- Important Interaction: beta-blockers may antagonize effects

slow and longer acting LABA; nocturnal asthma, exercise-induced asthma; inhibits late-phase allergen-induced bv after SABA wear off

Front 81

beta-agonists in general

Back 81

bronchodilators treat mild intermittent asthma; muscarinic Rc ag to relax sm inc cAMP; poss some COPD mostly asthma; B2 less cardiac effects but high doses can include B1

Front 82

Cabergoline

Back 82

Indicated for hyperprolactinemia disorders; either idiopathic or due to pituitary adenomas
- Agonist at DA D2 Rcs, more selective than Bromocriptine (less adverse effects) and Pergolide; longer DOA
Atypical Ergots: no ergot core, very small, bad bioavailability, differenct Rc selectivity; primarily Dopamine agonists

Front 83

Pergolide

Back 83

- Similar to Bromocriptine, selective for D2 and Serotonin, but 1000x more potent than Bromocriptine.
- Indicated for adjunct treatment of levodopa/carbidopa in management of Parkinson’s
- DA Rcs agonist at D1 and D2 Rcs, stimulates DA Rcs in Nigrostriatal System
- Added w/ L-DOPA may caused hallucinations in 14% of patients
Atypical Ergots: no ergot core, very small, bad bioavailability, differenct Rc selectivity; primarily Dopamine agonists

Front 84

name 2 atypical ergots

Back 84

cabergoline, pergolide

Front 85

naproxen

Back 85

NSAID; used to prevent a migraine and abort one
can be used for prevention and tx of migraine; block TX synthesis and plt agg so ↓ serotonin; continuously or intermittent; 1 wk before menses may prenvent.
Combination of acetaminophen, butalbital, and caffeine are effective

Front 86

Amitriptyline

Back 86

TCA is more potent inhibitor of serotonin reuptake and more effective; SE: drowsiness, tremor, and anticholinergic effects (dry mouth, burred vison and urinary retension)
phenelzine- monoamine oxidase inhibitor MAOI; can block serotonic degradation; occationally used in persons who fail to respond to other antidepressants; SE: hypertensive crisis if taken w/ tyramine foods
antidepresent used to prevent migraines

Front 87

propanolol

Back 87

BB- lack intrinsic sympathomimetic activity are effective like timolol and propanolol (more side effects than timolol)
MAO: may attenuate the 2nd phase by blocking VD by B2 and may ↓ plt agg
used for prophylaxis of migraines

Front 88

timolol

Back 88

BB- lack intrinsic sympathomimetic activity are effective like timolol and propanolol (more side effects than timolol)
MAO: may attenuate the 2nd phase by blocking VD by B2 and may ↓ plt agg
used for prophylaxis of migraines

Front 89

dihydropyridine drugs

Back 89

CCB -pine; can be used to prevent migraines
Dihydropyridine drugs: Felodipine,
amlodipine, nicardipine, nifedipine, nimodipine Dizziness, edema, gingival hyperplasia, headache, and tachycardia (reflex tachycardia). Serum levels of drug increased by azole antifungal agents, and grapefruit juice.

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nifedipine

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prophylaxis of migriane CCB
Dihydropyridine drugs: Felodipine,
amlodipine, nicardipine, nifedipine, nimodipine Dizziness, edema, gingival hyperplasia, headache, and tachycardia (reflex tachycardia). Serum levels of drug increased by azole antifungal agents, and grapefruit juice.

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Diltiazem

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migraine prophylaxis
Diltiazem, Verapamil (non-dihydropyridine; remember, more cardiac effects) Atrioventricular block, bradycardia, constipation, dizziness, edema, gingival hyperplasia, headache, and heart failure. Increases serum levels of carbamazepine, digoxin, and theophylline. Decreases serum levels of lithium.

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Verapamil

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migraine prophylaxis CCB
Diltiazem, Verapamil (non-dihydropyridine; remember, more cardiac effects) Atrioventricular block, bradycardia, constipation, dizziness, edema, gingival hyperplasia, headache, and heart failure. Increases serum levels of carbamazepine, digoxin, and theophylline. Decreases serum levels of lithium.
USED TO TREAT CLUSTER HEADACHE PREVENTS THEM TO REDUCE VC AS THE PRIMARY PHASE

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Gabapentin

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seizure disorders; postherpetic neuralgic; moderately effective in prevention; enhance GABA; some sedative effects
migraine prophylaxis

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riboflavin

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vit B2 can dec freq and duration of migriane attacks if taken daily >2 mo

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feverfew and ginger

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prophylaxis of migrianes

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Tramadol

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chronic pain; agonist at mu opioid Rc; inhibits NE and serotonin reuptake in CNS
abort migrianes

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Butorphanol

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agonist kappa opioid Rc; mixed at mu antagonist; nasal spray
aborts migrains

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Prochlorperazine

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antipsychotic aborting migraine IV

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Lysergic Acid Diethylamide (LSD

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“Lyserg-Saeure-Diaethylamid”
 Most potent hallucinogenic drug: 25 µg total dose (1.0 gram = 40,000 doses)
 Action: partial agonist at 5-HT1A autoreceptors on raphe cell neurons decreases neuronal activity and agonism at postsynaptic 5-HT1A and/or 5-HT2A/C receptors in visual processing centers (this gives us our hallucinations)
Amine Ergots: small ergots and better absorbed; more selective parial for serotonin

other CI: obstructive vascular or collagen disease; HTN, preg, psychosis

dopamine receptor agonist and serotonin agonist

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Ergonovine

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- Class:; uterine sm stimulation due to partial agonist effects at alpha 1-adrenergic and 5HT-2 Rc
- tx: Postpartum bleeding and labor induction when oxytocin-resistant
- Important Side Effects: ergotism (vasoconstriction) leading to gangrene and bowel infarction
- Important Interactions: Contraindicated in CV disease and pyschosis
Amine Ergots: small ergots and better absorbed; more selective parial for serotonin

other CI: obstructive vascular or collagen disease; HTN, preg, psychosis

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Methysergide

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for migraine prophylaxis; for diarrhea and malabsorption of carcinoid; antagonist of 5-HTA/C Rc; effects in 1-Amine Ergots: small ergots and better absorbed; more selective parial for serotonin 2 days and 1-2 days for effect to stop
***used to treat cluster headaches used in prevention reducing VC 1st phase

fibroplastic changes, pleural cavity and endocardial tissue not reversible

other CI: obstructive vascular or collagen disease; HTN, preg, psychosis

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Methylergonovine

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- Class: Ergot agonist at alpha-1 and 5HT-2 Rcs due to uterine sm stimulation
- tx: Postpartum bleeding and labor induction when oxytocin resistant
- Important Side Effects: ergotism (vasoconstriction) leading to gangrene and bowel infarction
- Important Interactions: Contraindicated in CV disease and pyschosis
Amine Ergots: small ergots and better absorbed; more selective parial for serotonin
prob less impt drug

other CI: obstructive vascular or collagen disease; HTN, preg, psychosis

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ergots side effects

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nl dose-diarrhea and N/V
high doses- CNS stim and hallucination think LSD

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contraindications of amine ergots

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obstructive vascular or collagen disease; HTN, preg, psychosis

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Amino Acid Ergots

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alkaloids most effective given early in migraine attack; SE: N/V, diarrhea, mm cramps, cold skin, paresthesias, and vertigo; CI in CV disease; may casued cerebral VC, ischemia, and rebound VD and headache for several days; intx w/ BB for peripheral ischemia; large, bad bioavailability, low potency; less selective; more widespread effects; can become additive

can add caffiene

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Dihydroergotamine

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intranasal and injectable
- Ergot Alkaloid (5HT agonist) Non-selective;
- Tx: ACUTE Moderate to severe migraine; DHE often w/ antiemetic drugs such as metoclopramide to prevent drug-induced N/V; in VD; pot fo rdependance, given for withdrawel w/ dysphria
- Important Side Effects: diarrhea, mm cramps, cold skin;
- Important Interactions: Contraindicated in CV disease and pyschosis
amino acid ergot

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Ergotamine

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(ergomar, ergostat, medihaler-ergotamine) parenteral, oral, and rectal (may stim nausea center); may have caffeine for VC too
- Class: ergot alkaloid (5HT ) agonist Nonselective
- tx: ACUTE Moderate to Severe Migraine; pot for dependance in VD phase; may b egiven to combat withdrawel in dysphoria
- Important Side Effects: ergotism (vasoconstriction) leading to gangrene and bowel infarction; stim a1-adrenoceptor to stim vascular smNOT use in CAD or peripheral vascular disease
- Important Interactions: Contraindicated in CV disease and pyschosis
AA ergot

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Ergotamine Tartrate

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AA ergot
- Class: Ergot agonist at 5HT Rc (5HT-1D/B)
- tx: acute treatment of moderate to severe migraine
- Important Side Effects: ergotism (vasoconstriction) leading to gangrene and bowel infarction
- Important Interactions: Contraindicated in CV disease and pyschosis
??? impt???

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Bromocriptine

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(first ergot that was truly DA selective)
- Used in Hyperprolactinemia (DA inhibits prolactin secretion), Parkinsons, and Acromegaly
- This is a DA D2 Rc Agonist, so it inhibits prolactin secretion w/ little effect on other pituitary hormones, replaces lost DA in Parkinson’s patient, and lowers blood levels of growth hormone in patients w/ acromegaly.

AA ergot; SE: N/V, diarrhea, mm crmaps, cold skin ect

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lithium

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used to prevent headaches at the 1st phase that reduces VC; used to treat cluster headaches

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cluster headaches

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primary headache;
severe, unilateral retro-orbital; cluster over time, min sensory input impacts; searing burning pain behind one eye w/ fast onset; 15 min-3 hrs at same time each day; agitated w/ pressure to orbit or hurt them selves to distract form pain; lithium, methy sergide and verapamil prevent these and DHE, ergotamin, glucocorticoids, lidocains, O2 and sumatriptan abort them

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2 phases of migraines

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2 phases:
Cerrebral VC (and ischemia; release serotonin (anti plt drugs work)) followed by cerebral VD (long cerebral VD and pain; trigeminal neruovascular system release vasoactive peptides like substance P and calitonic gene)
(primary headache)

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migraine is

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Moderate or severe, often unilateral, usually pulsatile; occur with or without aura; often w/ powerful sensory input impacts

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drugs to prevent migraine as prophylaxis

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β-Adrenoceptor antagonists, anticonvulsants, antidepressants, calcium channel blockers, NSAIDs, and serotonin 5-HT2 receptor antagonists

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drugs to abort migraines

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DHE, ergotamine, isometheptene, NSAIDs, tramadol, and triptans

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Tension headaches

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Mild or moderate, bilateral, nonpulsatile; exert band-like pressure; correct cervical or dental alignment or visual error

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treat tension headaches to prophylax

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amitriptyline

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treat tension headaches to abort w/

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mm relaxants and NSAIDs

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secondary headaches

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vary depend on underlying cause; disease; no drugs to treat

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serotonin Rc agonists treat

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sumatriptan and ergotamine; treat migraine to abort in 2nd phase

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propanolol tx

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prevnet migraines as BB

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timolol

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prevents migrains BB

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NSAIDs

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prevent and abort migraines; naproxen and fenoprofen

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nimodipine

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CCB; prevent migraines and cluster headaches

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valproate

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anticonvulsant for migraine prophylxis; onset efficacy 2-3 wks; somewhat shorter; SE: sedation, tremor, weight gain
3 antidepressants: downregulate postsynaptic serotonin Rc; inc firing of serotonin neurons

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ergots amines

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better abosorbed; small
LSD, ergonovine, methyergonovine, methysergide

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ergots aminoacid

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ergotamine, DHE, bromocriptine, ergoloids; large, bad F; low potency, need large dosese

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atypical ergots

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pergolide, cabergoline; no ergot core; dopamine based; very small diff Rc selectivity

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epinephrine

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nonselective a and b; used in emergencies; poss CV rxn; a1 for bvs and B1 in heart

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isoproterenol

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B1 and 2 agonist; inc HR, tachy
simm to adrenerline; used in bradycardia; tx torsades