Term
| What are the 4 Histamine Inhibitors & Physiological Antagonists |
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Definition
B-Adrenoceptor Agonists
Cromolyn
Epi
Nedocromil |
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Term
| What are 6 1st Generation H1 -Receptor Antagonists |
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Definition
Cyclizine
Cyproheptadine
Dimenhydrinate
Diphenhydramine
Meclizine
Promethazine |
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Term
| What is the the primary 2nd generation H1 -Receptor Antagonists |
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Definition
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Term
| What 4 H2 -Receptor Antagonists |
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Definition
Cimetidine
Famotidine
Nizatidine
Ranitidine |
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Term
|
Definition
Buspirone
Dihydroergotamine
Ergonovine
Ergotamine
LSD
Metoclopramide |
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Term
|
Definition
Eletriptan
Frovatriptan
Naratriptan
Sumatriptan
Zolmitriptan |
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Term
| What are 8 5-HT Antagonists |
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Definition
Bromocriptine
Butyrophenones
Cyproheptadine
Methysergide
Ondansetron
Phenoxybenzamine
Phenothiazines
Ritanserin |
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Term
Name 6 Prostaglandins
Hint: Prostaglandins have "prost" in the name |
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Definition
Alprostadil
Carboprost Tromethamine
Dinoprostone
Epoprostenol
Latanprost
Misoprostol |
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Term
| What are the Eicosanoid (PG) inhibitors |
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Definition
*Cromolyn
Glucocoticoids
Montelukast
NSAIDS
Zafirlukast
Zileuton
*Cromlyn is also a Histamine Inhibitor |
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Term
| Where is most of Histamine Stored |
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Definition
| It is sequestered and bound in the granules of mast cells or basophils |
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Term
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Definition
| Binds adn stimulates H1 - H4 receptors |
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Term
| Where are H1 -Receptors Located |
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Definition
| Smooth Muscle, Endothelium, and brain (post-synaptic membrane) |
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Term
| Does H1 -receptors Inhibit or Stimulate IP3 /DAG? |
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Definition
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Term
| Where are the H2 -receptors located |
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Definition
| Gastric mucosa, cardiac muscle, mast cells, and brain (post-synpatic membrane) |
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Term
| What is the effect of H2-receptors on cAMP and IP3/DAG |
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Definition
| They stimulate both cAMP production and IP3/DAG |
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Term
| In neurons, which receptor is a powerful stimulant of sensory nerve endings mediating pain & itching |
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Definition
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Term
| Which receptor control respiratory neurons |
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Definition
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Term
| Which receptor is resonsible for contraction of the uterus |
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Definition
H1
*Spontaneous abortion can occur in women suffering from anaphylactic attack due to excess Histamine release |
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Term
| Which receptor is responsible for bronchoconstriction |
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Definition
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Term
| Which receptor is a powerful stimulant of gastric acid secretion and induction of pepsin and intrinsic factor |
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Definition
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Term
| Which receptor cause contraction of intestinal smooth muscle |
|
Definition
H1
*Large doses may induce Diarrhea
*Secretion stimulated in both S.I. & L.I. |
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Term
| Which receptor increases heart rate with direct infusion of histamine |
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Definition
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Term
| Which receptor increases contractility and pacemaker rate |
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Definition
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Term
| Which receptor decrease Atrial contractility |
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Definition
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Term
| What is the triple response? What receptor is Mostly responsible |
|
Definition
Reddening of skin
Edematous wheal
Flares
* Mainly H1 mediated |
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Term
| What are the 3 cell types involved in the triple response |
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Definition
Microcirculation vessel smooth muscle cells
Capillary/venular endothelium
Sensory neurons |
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Term
| Injection of Histamine decreases SP & DP, with low dose admin, what receptor is activated? what receptor activated with High dose admin? |
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Definition
H1 activation along with NO (with low doses)
H2 (with high doses) |
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Term
| Histamine induces edema due to its effects on post-capillary vessels, what receptor is responsible? |
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Definition
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Term
| Clinical use of Histamine |
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Definition
| Test for Bronchial Hypersensitivity |
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Term
| Adverse effects of Histamine |
|
Definition
Flushing
Hypotension
Tachy
Headache
wheals
Bronchoconstriction
GI Upset
*Scombroid fish poisoning |
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Term
| What are the Contraindications for Histamine |
|
Definition
Asthma
Active ulcer disease
GI Bleeding |
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Term
| What is the typical action H1 antagonists |
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Definition
| It is a traditional antihistamine |
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Term
| What are H2 antagonists use to treat? |
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Definition
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Term
| What is a strong effect of 1st generation agents |
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Definition
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Term
| Why does 2nd generation Histamine Antagonists have less of a sedative effect then 1st generation |
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Definition
| Because they have less complete distribution into the CNS |
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Term
| What are 2 differences btw 1st and 2nd generation Histamine Antagonists |
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Definition
1st generation enter the CNS, 2nd's Do NOT
1st genaration are more Lipid Soluble (could account for why they enter the brain) |
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Term
| Which generation of Histamine Antagonists are longer acting |
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Definition
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Term
| What is MOA of H1 receptor Antagonists |
|
Definition
Reversible competitive inhibition of the receptors
*More are antagonists, but some are inverse agonists |
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Term
| What other receptors does 1st generation agents effect |
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Definition
| muscurinic cholinergics, α-adrenoceptor, serotonin, local anesthetic |
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Term
| What are the effects mediated by inhibiting H1receptors |
|
Definition
Inhibition of edema and itching
inhibit histamine induced hypotension
antinausea & antiemetic
inhibit bronchiolar & GI smooth muscle contraction |
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Term
| What are the therapeutic uses of H1 receptor Antagonists |
|
Definition
Allergic rxns -*moreeffective if given b4 exposure
Motion sickness & Vestibular disturbance
Parkinsons |
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Term
| Adverse effects of H1receptor Antagonists |
|
Definition
Sedation - *Only 1st gen
Urinary retention and blurred vision - *only 1st gen due to antimuscurinic effects
Drug Allergy |
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Term
| What are the Toxic effects of H1receptor Antagonists |
|
Definition
Hallucination
excitement
*anything lead to uncoordination
tachy
dry mouth
cardiorespiratory collapse
fever coma
death |
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Term
| Contraindications of H1 receptor Antagonists |
|
Definition
Use with CNS depressing agents while driving or operating machinery - *only with 1st generation agents
Use with muscurinic & α-blocking drugs (additive effects)
Children, elderly
Pregnancy |
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Term
| Which H2receptor Antagonist has a small 1st pass effect |
|
Definition
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Term
| Where are H2receptor Antagonists distributed? |
|
Definition
| All organs including the brain |
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Term
| What is the clearance of H2receptor Antagonist? |
|
Definition
Renal, hepatic, and GFR
*dose reduction in pt with moderate to severe renal/hepatic insufficiency |
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Term
| What is the MOA of H2receptor Antagonists |
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Definition
| Competitive inhibitors of receptors on gut parietal cells |
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Term
| Overall what is the pharmacological effect of H2receptor inhibition |
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Definition
| Overall the effects is reduction of digestive enzyme secretion |
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Term
What other important role does Cimitidine play
Hint- CYP450 |
|
Definition
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Term
| What are the therapeutic uses of H2receptor Antagonists |
|
Definition
GERD (b/c reduces GI secretions)
Peptic Ulcer (b/c nocturnal acid suppression)
Esophagitis
Bleeding due to gastritis |
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|
Term
| What kind of ulcers are treatment with H2receptor Antagonists contraindicated? |
|
Definition
| Ones that are cause by H.Pylori or NSAID usage |
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Term
| Adverse effects H2receptor Antagonists |
|
Definition
Diarrhea, headache, fatique, constipation, myalgia
change in mental status (esp in elderly w/ renal or hepatic dysfunction) |
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Term
| What are specific adverse effects of Cimetidine? |
|
Definition
Blocks DHT androgen receptor, inhibits estradiol, and increses serum prolactin
*Long term use can lead to gynecomastia, galactorrhea, loss of libido, and impotence |
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Term
| Contraindication of H2receptor Antagonists |
|
Definition
Use with Antacids (these reduce absorption of the antagonists)
Use of Cimetidine with drugs metabolized via P450 (drugs include: WARFARIN, anti-seziure, anti-epilepsy, asthma, etc.)
Use with Alcohol
Renal/Hepatic disease
Pregnancy |
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Term
| Where is most of 5-HT stored |
|
Definition
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Term
| What areas are 5-HT clinically involved in? |
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Definition
| Depression, Anxiety, *Migraines* |
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Term
| What are two major 5-HT receptors? Where are they located? What is their mechanism? |
|
Definition
5-HT1B- Substantia nigra, globus pallidus, Basal Ganglia- Gi, dec cAMP
5-HT1D- Brain- Gi, dec cAMP |
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Term
| What is the Drug of Choice (DOC) for Cluster headaches |
|
Definition
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Term
| What is the MOA of Triptans |
|
Definition
| Selective agonists for 5-HT1B & 5-HT1D |
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Term
| What effect does Triptans Mediate? |
|
Definition
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Term
| What are the pharm effects of Triptans |
|
Definition
Inhibit release of vasodilating peptides (CGRP, Sub P) from trigem nervers- *Imp in Migraine Headaches
Induce Vasoconstriction of cerebral vessels of trigeminovascular system - *Imp in Migraine headaches
*See the patter IMPORTANT IN MIGRAINES |
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Term
| Therapeutic use of Triptans? |
|
Definition
mmmmm....IMPORTANT IN MIGRAINES!!
DOC in Migraines |
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|
Term
| Adverse Effects of Triptans |
|
Definition
Altered sensations - tingling, warm, dizzy, etc
Injection site rxns
Arrythmias
MI - in predisposed |
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|
Term
| Contraindications of Triptan |
|
Definition
Angina
CAD
Severe hepatic or renal impairment
Peripheral vascular syndromes (nara & eletriptan)
Wolff-Parkinsons-White Syndrome (zolmitriptan)
Use with other 5-HT agonists, SSRIs or MAOIs |
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|
Term
What is Buspirone use to Tx
Hint: What med student have b4 exams |
|
Definition
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|
Term
What is Metoclopramide used to Tx?
Hint: Bad Restuarant/Shack Attack |
|
Definition
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Term
| What are the symptoms of Ergotism? |
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Definition
| Ergotism is ergot poisoning effects inc: dimentia with hallucinations, prolonged vasospasms (may result in gangrene) & stimulation of uterine smooth muscle (spontaneous abortion may result) |
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|
Term
What are the Ergot drugs?
|
|
Definition
LSD
Ergonovine
Methylergonovine
DihydroErgotamine
Ergotamine
Bromocriptine |
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|
Term
| What enhances the asorption and bioavailability of ergotamine? |
|
Definition
| Concommitant use with caffeine |
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|
Term
| What is the oral bioavailability of LSD and ergonovine? |
|
Definition
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Term
| Mechanism of Action of Ergot Alkaloids? |
|
Definition
Depending on agent, dose & tissue.
LSD (CNS), Ergonovine, & Dihyroergotamine = AGONISTS
LSD (Peripheral), Bromocriptine, & Methysergide = ANTAGONISTS
Ergotamine & Methysergide = PARTIAL AGONISTS
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|
|
Term
What are the therapeutic doses of Ergot Alkyloids?
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|
Definition
Migraines - must give at 1st sign of attack (DOC Ergotamine and dihydroergotamine)
Hyperprolactinemia (Bromocriptine)
Postpartum Bleeding- VC the BVs only for late uterine bleeding (Ergonivine)
Parkinsons (Bromocriptine)
Dx of Variant Angina (Ergonovine) |
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Term
| Adverse effects of Ergot Alkyloids |
|
Definition
Diarrhea, n/v = most common
Narrow therapeutic index
Prolonged vasospasm
Bowel infarction
Uterine cramping (ergonovine)
Drowsiness
CNS stimulation & Hallucintations |
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Term
| Contraindications with Ergot Alkyloids |
|
Definition
Cerebrovascular disease
Obstructive vascular disease
Collagen disease
Pregnancy |
|
|
Term
What is Phenoxybenzamine used to manage
*hint: angry kid with increased catecholamines |
|
Definition
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|
Term
| What is Cyproheptadine used for? |
|
Definition
| Prevents smooth muscle effects & tx smooth muscle manifestation of carcinoid tumor and cold induced urticaria |
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|
Term
|
Definition
| Alters bleeding time and reduces thromboxane formation by altering platelet function |
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|
Term
| What is Ondansetron use for? |
|
Definition
| Tx n/v associated with surgery and cancer chemo |
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|
Term
| What are Phenothiazines & Butyrophenones use for? |
|
Definition
|
|
Term
| What are features of Tension Headaches? |
|
Definition
Family Hx, Females, Bilateral, precipitated by stress, dull persistant pain, worsen with emotional disturbance, Anorexia an associated symptom
.5 hr - 7 dy duration |
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|
Term
| What are features of Cluster headaches? |
|
Definition
No Fam Hx, Men, during sleep, behind or around eye, excruciating sharp steady pain, 15-90min attack
Associate symptoms: edema below eye, sweating, flushing, rhinorrhea, lacrimation and papillary changes |
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|
Term
|
Definition
Fam Hx, Females, variable onset, unilateral, pulsating throbbing pain, 2-72h attack
Assoc symptoms: visual auras, scintillating scotomas, pallor, anorexia, n/v |
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|
Term
|
Definition
Mild/Mod - NSAIDS/Acetominophen
Mod/Severe- Ergoline drugs; NSAIDS, Triptans, Opioids
Prophylaxis - Anticonvulsants, B-blockers, NSAIDS |
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|
Term
| What are the 2 key enzymes in the Cox Pathway |
|
Definition
Cox-1- Constuitively expressed
Cox-2 - inducible expression via shear stress, growth factors, cytokines, and tumor promotors. Involved mainly in inflammation, fever production, and cancer |
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|
Term
|
Definition
Bind to specific cell surface receptors that are cell type & density dependent
Signaling mechanisms include activation or inhibiton of cAMP, IP3/Dag, PLC, and Rho GTPase |
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|
Term
Therapeutic Use of Alprostadil?
|
|
Definition
Erectile Dysfunction
Maintenance of the patency of fetal ductus arteriosus |
|
|
Term
| Adverse Effects of Alprostadil? |
|
Definition
Penile Pain, prolonged erection, priapism
In neonates: apnea, brady, hypotension, hyperthermia, hyperpyrexia |
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|
Term
| What is the clinical use for Carboprost Tromethamine? |
|
Definition
Induction of 2nd trimester abortion
Control postpartum hemmorrhage |
|
|
Term
| What are the adverse effects of Carboprost Tromethamine? |
|
Definition
| Vomiting, diarrhea, bronchoconstriction, temp elevation |
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|
Term
| What is the only form of admin for Dionoprostone? |
|
Definition
|
|
Term
| What is the MOA of Dinoprostone? |
|
Definition
Stimulates induction of uterine contractions
Effects cervical collagenase |
|
|
Term
| What is the clinical use of Dinoprostone? |
|
Definition
Induction of 2nd trimester abortion
Missed abortion
Benign Hydatiform mole
Ripening of cervix for the induction of labor in pt at or near term |
|
|
Term
What are the adverse effects of Dinoprostone?
|
|
Definition
|
|
Term
| What are the therapeutic uses of Epoprostenol? |
|
Definition
| Tx of primary pulmonary hypertension |
|
|
Term
| What are the adverse effects of Epeprostenol? |
|
Definition
| Flushing, headache, hypotenstion, nausea, diarrhea |
|
|
Term
What is the therapeutic use of Latanoprost?
Hint: Opthalmic admin |
|
Definition
| Open angel glaucoma b/c of its ocular hypotensive effects |
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|
Term
| Adverse effects of Latanoprost? |
|
Definition
| Irreversible brown pigmentation of the iris and eyelashes, drying of eyes, and conjuntivitis |
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|
Term
| What is the route of Admin for Misoprostol |
|
Definition
|
|
Term
| What is the therapeutic use of Misoprostal |
|
Definition
Admin w/ RU-486 to induce early abortion
Tx of NSAID induced peptic ulcer |
|
|
Term
| What are the adverse effects of Misoprostol |
|
Definition
Cramping, diarrhea, sepsis (via vaginal route)
Bone pain and hyperostosis in pt with liver disease with long-term PGE tx |
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|
Term
| What is Alprostadil used for clinically & therapuetically |
|
Definition
Penile injection stimulant - clinically
Erectile dysfunction (2nd line of tx) & maintain patency of fetal ductus arteriosus in neonates - Therapeutically |
|
|
Term
| Eicosinoid Inhibitors are used to treat asthma, what drugs are involved and how do they work |
|
Definition
Zifirlukasts - LT receptor inhibitot
Zileuton - LOX inhibito
GCC- inhibit all econsinoid pathways
Cromyln- Inhibit eicosinoid release |
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|
Term
| How does Cox inhibitors aid in closing a delayed ductus arterious |
|
Definition
Block PGE2 synthesis
*Remember Alaprostidil is used to maintain DA so by blocking this you allow it to close |
|
|
Term
| Dysmenorrha is treated with what Eicosinoid Inhibitors? |
|
Definition
| NSAIDS....aspirin not as effective here; done by blocking PGE2 & PGF2α |
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|
Term
| What is the role of Eicosinoids Inhibitors in inflammation |
|
Definition
| Aspirin & Cox Inhibitors are used to prevent/reduce inflammatory conditions i.e arthritis |
|
|
Term
| What is the role of Eicosinoid inhibitors in thrombosis |
|
Definition
| Low dose aspirin selectively and irreverisbly inhibits platelet COX-1 this block thrombosis |
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