Download Autocoids

Antihistamines
Serotonin Agonists
Histamine Antagonists
• H 1 receptors
• inhibit smooth muscle
contraction
• decrease wheal,
flare,and itch
• decrease secretions:
salivary and lachrymal
• CNS: sedation
• H 2 receptors
• inhibit gastric acid
secretion
• decrease content and
volume of gastric juice
• fasting, food
stimulated and
nocturnal
H 1 antagonists
• Relief of manifestations of immediate-type
hypersensitivity reactions
– allergic rhinitis
– cold remedies
• newer agents “selective” for peripheral H 1
receptors
– less sedation (dose dependant)
Antihistamine Products
• sedating
– diphenhydramine
(Benadryl)
– chlorpheniramine
(Chlor-Trimeton)
• non-sedating
– fexofenadine (Allegra)
– loratadine (Claritin)
– cetirizine (Zyrtec)*
• * metabolite sedating
Sedation
• dose related even for newer agents
• most common ingredient in OTC sleep aids
Children’s Formulations
• Most available as syrups
• Allegra
– 30 mg tab
• Claritin
– 10 mg Redi-tab (fast dissolve)
Role of Antihistamines in the Treatment of
Allergic Rhinitis
Nasal Steroids vs. Antihistamines
January 2001
UCDHS Adult Allergic Rhinoconjunctivitis Guidelines
Rhinitis Definition
Nasal Discharge
Blockage
Sneeze/Itch
Moderate Seasonal or Moderate Perennial
Allergen Avoidance
Rhinocort , or Nasonex: Nasal Inhalation
non-sedating antihistamine, ocular medication "as needed"
Severe Long Seasonal or Severe Perennial
Allergen Avoidance and Nasal Steroids with
Daily non-sedating antihistamine
topical antihistamine for conjunctivitis if needed
2 sprays each nostril bid (Rhinocort), qd (Nasonex)
Allegra 60 mg bid for two weeks
then "as needed"
naphazoline opthalmic "as needed"
Rhinocort 2-4 sprays each nostril twice a day,
Nasonex 2 sprays each nostril daily
with Allegra 60 mg twice a day and if needed
lodoxamide (Alomide)1-2 drops affected eye(s) 4x day
Treatment Failures
Evaluate patient compliance and inhaler technique
Consider alternative nasal steroid
continue Allegra "as needed"
For Treament Failures
Evaluate patient compliance and inhaler technique
Use alternative nasal steroid
severe rhinorrhea: Atrovent Nasal 2 sprays each nostil 3-4x day
HealthNet: Nasonex, Nasacort
Pacificare: Rhinocort, Nasonex, Nasarel
REFER
TO
ALLERGIST
IMMUNOTHERAPY
WHA: Rhinocort, Nasonex, Nasacort AQ
Approved UCDMG P&T Committee January 2001
Reviewed by: T. Albertson S. Teuber, M. E. Gershwin, R. Mowers, J. Fischer
HealthNet Jan-Jun 2002
Label_name
ALLEGRA
ALLEGRA-D
CLARINEX
CLARINEX
TAB 5MG
CLARITIN
CLARITIN-D 12 HOUR
CLARITIN-D 24 HOUR
FLONASE
NASACORT
NASACORT AQ
NASALIDE
NASAREL
RHINOCORT
RHINOCORT AQUA
ZYRTEC
ZYRTEC-D
Total Average of Ing_cost
Total Sum of Ing_cost
Total Number of Rx
Data
Total
Average of Ing_cost
63.59
Sum of Ing_cost
246,090.63
Number of Rx
3,870
Average of Ing_cost
55.34
Sum of Ing_cost
3,209.82
Number of Rx
58
Average of Ing_cost
54.37
Sum of Ing_cost
69,318.89
Number of Rx
1,275
Average of Ing_cost
55.63
Sum of Ing_cost
278.13
Number of Rx
5
Average of Ing_cost
76.42
Sum of Ing_cost
267,921.14
Number of Rx
3,506
Average of Ing_cost
78.77
Sum of Ing_cost
12,131.11
Number of Rx
154
Average of Ing_cost
80.74
Sum of Ing_cost
19,862.94
Number of Rx
246
Average of Ing_cost
53.52
Sum of Ing_cost
73,590.60
Number of Rx
1,375
Average of Ing_cost
51.04
Sum of Ing_cost
9,237.88
Number of Rx
181
Average of Ing_cost
47.78
Sum of Ing_cost
44,821.44
Number of Rx
938
Average of Ing_cost
42.63
Sum of Ing_cost
255.77
Number of Rx
6
Average of Ing_cost
24.26
Sum of Ing_cost
121.30
Number of Rx
5
Average of Ing_cost
37.46
Sum of Ing_cost
13,074.74
Number of Rx
349
Average of Ing_cost
55.24
Sum of Ing_cost
5,192.84
Number of Rx
94
Average of Ing_cost
50.21
Sum of Ing_cost
41,826.46
Number of Rx
833
Average of Ing_cost
49.40
Sum of Ing_cost
493.99
Number of Rx
10
62.57
807,427.68
12,905
other routes of administration
• azelastine (Astelin)
– nasal spray
– allergic rhinitis
– decrease side effect
profile
• Bitter amine taste
• sedation (systemic
absorption)
• olopatadine (Patanol)
• emedastine (Emadine)
• ophthalmic antihistamine
H1
• allergic conjuctivitis and
itching
• headache, taste perversion,
abnormal dreams
H 2 Antagonists
• Therapeutic Indications
–
–
–
–
–
–
duodenal and gastric ulcer
gastroesophageal reflux disease (GERD)
erosive esophagitis
hypersecratory conditions
heart burn, indigestion, sour stomach
multidrug regimen for the eradication of
H.Pylori in peptic ulcer disease
UC Davis Primary Care Adult Tx: GERD
Diagnosis
Gastroesophogeal Reflux Disease
Severe GERD
(Erosive esophagitis
Barrett's esopagus,
esophageal stricture)
Approve for long term
maintance therapy
PPI
Mild to Moderate GERD
(Reflux esophagitis)
Surgery
Drug
Protonix® 40 mg
Aciphex® 20 mg
Prevacid® 30 mg
Nexium® 20 mg
Prilosec® 20 mg
8 weeks therapy
"Step Up" Start with High Dose H2
cimetidine 800 mg bid
ranitidine 150 mg bid
Beck IT et al. The Second Canadian
Consensus Conf. on Management of Patients
with GERD. Can J Gastroenterol 1997;11
suppl B 7-20.
Katz PO. Treatment of GERD: Use of
Algorithms. Am J Gastroenterol
1999;94(11)suppl:3-10.
Improvment
No Improvment
Reduce to maintance dose
cimetidine 400 mg hs
ranitidine 150 mg hs
Protonix 40 mg daily
Aciphex 20 mg daily
Prevacid 30 mg daily
Prilosec/Nexium 20 mg daily
Re-evaluate patient symptoms
at 16 weeks total therapy
Re-evaluate patient symptoms
at 16 weeks total therapy
Reviewed by; T. Albertson, J. Lee, J. Fischer, R. Mowers
discontinue drug
continue H2 maintance
Improvement
No Improvement
discontinue drug therapy
change to H2 maintance therapy
Refer to GI Specialist
UCDMC P&T Committee January 2002
June 2001
AWP/ea
3.00
3.70
3.88
3.99
4.15
HealthNet Jan-Jun 2002
Label_name
ACIPHEX
Data
Total
Average of Ing_cost
119.73
Sum of Ing_cost
275,734.11
Count of Pt_first_name
2303
CIMETIDINE
Average of Ing_cost
8.96
Sum of Ing_cost
7,179.47
Count of Pt_first_name
801
CIMETIDINE HCL
Average of Ing_cost
38.36
Sum of Ing_cost
191.82
Count of Pt_first_name
5
FAMOTIDINE
Average of Ing_cost
27.44
Sum of Ing_cost
2,908.76
Count of Pt_first_name
106
NEXIUM
Average of Ing_cost
115.34
Sum of Ing_cost
7,843.10
Count of Pt_first_name
68
PREVACID
Average of Ing_cost
119.92
Sum of Ing_cost
17,627.56
Count of Pt_first_name
147
PRILOSEC
Average of Ing_cost
139.62
Sum of Ing_cost
73,021.10
Count of Pt_first_name
523
PROTONIX
Average of Ing_cost
88.35
Sum of Ing_cost
172,897.16
Count of Pt_first_name
1957
RANITIDINE TAB 150MG
Average of Ing_cost
6.69
Sum of Ing_cost
100.31
Count of Pt_first_name
15
RANITIDINE TAB 300MG
Average of Ing_cost
7.57
Sum of Ing_cost
30.29
Count of Pt_first_name
4
RANITIDINE HCL
Average of Ing_cost
10.26
Sum of Ing_cost
21,961.43
Count of Pt_first_name
2140
Total Average of Ing_cost
71.82
Total Sum of Ing_cost
579,495.11
Total Count of Pt_first_name
8069
Adverse Reactions
• low incidence of side effects
• headache and fatigue - 1%
• cimetidine
– highest incidence of gynecomastia (1- 4%)
– P450 drug interactions
• decrease digoxin levels
• increase flecainide activity
Serotonin 5-HT1 agonists
• Treatment of Migraine with or without aura.
• Acute treatment of Cluster headaches.
• Drugs are combination of 5-HT (1A, 1B,
1D, 1E, 1F, 7)
• No activity at 5HT 2-4 receptors,
adrenergic, muscarinic, dopaminergic
Mechanism of Action
• Stimulation 5HT-1 receptors in extracerebral and
intracranial blood vessels results in
vasoconstriction. Also seen is an inhibition of
neuropeptide release and decreased transmission
in trigeminal pain pathways.
• It is thought cranial vessel dilation induced by
release of vasoactive peptides from sensory nerve
endings in an active trigeminal system my be a
root cause of Migraine.
Prototype agents
• sumatriptan (Imitrex)
– Tablets, nasal spray, injection
• rizatriptan (Maxalt)
• Several others
Common adverse events
• Generally well tolerated
• Events with 5% rate: paresthesia, nausea,
dizzsiness, fatigue, dry mouth, headache,
flushing
• Rare but serious events: cardiac events with
fatalities, cerebrovascular events with
fatalities (hemorrhage, stroke, others)
Rebound headache
• The risk of rebound headaches increases
with the number of doses taken.
• Patient information:
– Take as soon as possible
– Second dose may be taken if no response in 2
hours
– Limit injections to 2 per 24 hours
– Contact MD before taking additional doses if
no response
• Other drugs for Migraine Treatment
• Ergot alkaloids such as dihydroergotamine
(Migranal, DHE 45)
• Migraine Prophylaxis
–
–
–
–
Beta blockers
Calcium channel blockers
NSAID
Valproate