Antihistamine and Drugs for

Pneumonia
Andi Alfia MT
Department of Pharmacology, Medical Faculty
Universitas Tadulako
2019

1
 Antihistamines

4 types of histamine receptors (H1-H4)  H1 and H2 being

most widely expressed

MoA of H1 receptor antagonists

• Inhibit smooth muscle constriction in blood vessels &

respiratory & GI tracts
• Decrease capillary permeability
• Decrease salivation & tear formation

2
3
4
Before After

5
 Antihistamines (Cont’d)

First-generation H1 receptor antagonists

• Non-selective/sedating
• Bind to both central & peripheral H1 receptors
• Usually cause CNS depression (drowsiness,
sedation) but may cause CNS stimulation (anxiety,
agitation), especially in children
• Also have substantial anticholinergic effects

6
 Antihistamines (Cont’d)
Dosage
Drug
Adult Child
Chorpheniramin 4 mg q4-6hr, max: 24 mg 1-2yrs: 1 mg twice daily
e (4 mg tablet, daily 2-12yrs: 1- 2 mg q4-6h, Max:12 mg
2mg/ml Elixir & daily
expectorant)
Hydroxyzine (25 25 mg at night; 25mg 6 months-6yrs: 5-15 mg daily; 50
mg tablet) three to four times daily mg daily in divided dose if needed
when necessary >6yrs: 15-25 mg daily; 50-100 mg
daily in divided dose if needed

Diphendramine 25-50 mg q4-6h 6.25-25 mg q4-8 hr ( >1 yr)

(10 mg/5ml Elixir)

7
 Antihistamines (Cont’d)

Dosage
Drug (Cont’d)
Adult Child
Promethazine 25 mg at night; 25 mg 2-10yrs: 5-25 mg daily in 1
(10 & 25 mg twice daily if needed to 2 divided dose
tablets, 5mg/5ml
Elixir)

Azatadine (1 mg 1 mg twice daily 1-12 yrs: 0.25-1 mg twice

tablet) daily

8
 Antihistamines (Cont’d)
Adverse effects:
• Sedation
• Dry mouth
• Blurred vision
• GI disturbances
• Headache
• Urinary retention
• Hydroxyzine is not recommended for pregnancy &
breast-feeding
• Lowered seizure threshold
Overdose
• ≈ anticholinergic signs
9
 Antihistamines (Cont’d)
Second-generation H1 receptor
antagonists

• Selective/non-sedating
• Cause less CNS depression because they are
selective for peripheral H1 receptors & do not
cross blood-brain barrier
• Longer-acting compared to first-generation
antihistamines

10
 Antihistamines (Cont’d)
Drug Dosage
Adult Child
Cetirizine (Zyrtec) 10 mg daily 5 mg daily / 2.5 mg
twice daily (2-6 yrs)
Desloratadine (Aerius) 5 mg daily 1.25 mg daily (2-5 yrs)
2.5 mg daily (6-11yrs)
Fexofenadine (Telfast) 120-180 mg daily Not recommended

Loratadine (Clarityne) 10 mg daily` 5 mg daily (2-5 yrs)

11
12
 Antihistamines (Cont’d)
Adverse effects:
• May cause slight sedation, headache, fatigue
• Some antihistamines may interact with antifungal, e.g.
ketoconazole; antibiotics, e.g. erythromycin; prokinetic
drug-- cisapride or grapefruit juice, leading to
potentially serious ECG changes e.g. Terfenadine

Overdose

• tachycardia, drowsiness, agitation, gastrointestinal

effects and headache

13
 Antihistamines (Cont’d)

Used for

• Allergic rhinitis (oral, topical)

• Allergic conjunctivitis (oral, topical)
• Acute allergic reactions (non sedating)
• no role in the acute treatment of anaphylaxis
• Urticaria
• Colds and flu
• Prevention of motion sickness

14
 Antihistamines (Cont’d)
Conclusion

• They have a role in treating allergic

rhinitis, allergic conjunctivitis and
urticaria.
• The older antihistamines caused sedation
so they have now been superseded by
newer, less sedating drugs.

15
DRUGS FOR PNEUMONIA

16
 Introduction
Definition
• An infection that inflames the air sacs in
one or both lungs
Sign & Symptoms
• Cough
• Purulent sputum
• Chestpain
• Dyspnea
• PE: T > 38°C, consolidation, ronkhi
• LE: AL > 10000 uL or <4500 ul
• Abnormality of radiological
presentation
17
 Introduction (Cont’d)
Etiologies

18
 Treatment
Oxygenation
Empirical antibiotic (hypoxemia) 
(ASAP) specific noninvasive
ventilation

Fluid resucitation
Antipiretic
(hypotension)

19
 ADULT

20
 ADULT

21
 Macrolides
Irreversibly bind the 50S subunit.
• Binding site is in close proximity to the binding sites of
lincomycin, clindamycin and chloramphenicol.
Erythromycin (Oral)
• Gram positives: Staph.(MRSA is resistant), Strep., Bordetella,
Treponema, Corynebacteria.
• Atypicals: Mycoplasma, Ureaplasma, Chlamydia
Clarithromycin (Oral)
• Similar to erythromycin.
• Increased activity against gram negatives (H. flu, Moraxella)
and atypicals
Azithromycin (IM, Oral)
• Decreased activity against gram positive cocci.
• Increased activity against H. flu and M. cat.
 Beta Lactams

• B-lactams inhibit
transpeptidase.

• Only effective against rapidly

growing organisms that
synthesize peptidoglycan
(Ineffective against
mycobacteria.)

• Spectrum of activity: very

wide, anaerobes
 ß-Lactams
ß-Lactams
Penicillin
Narrow Spectrum
Cephalosporin •Benzylpenicillin (Penicillin G)
•Cefazolin, •Phenoxymethylpenicillin (Pen V)
Cefadroxil, Broad Spectrum
Cefalexin •Amoxicillin/Co-amoxiclav
•Cefuroxime •Ampicillin
•Cefixim,
Cefoperazon,
Carbapenem
Cefotaksim, •Meropenem
Cefpirom,
Cefpodoksim
proxetil,
Ceftazidim,
Ceftriaxon
•Cefepim
 Cephalosporins
Third Generation Fourth Generation
• Spectrum: gram negative > • Cefepime (IV)
gram positive.
• Active against Strep, Staph
• Ceftriaxone (IM/IV;),
Cefotaxime (mssa), aerobic gram
– Useful for meningitis. negatives (enterobacter, e.
– Ceftriaxone used for highly coli, klebsiella, proteus and
resistant and multi drug pseudomonas)
resistant strep pneumo
along with vancomycin.
• Ceftazidime active against
pseudomonas.
26
27
 CHILDREN

28
 CHILDREN

29
 ANTIVIRAL

30
 Oseltamivir & Zanamivir
MoA
• Neuraiminidase inhibitor  interfere with release of preogeny
influenza virus from infected host cells
Used for
• Influenza A & B
• Prophylaxis -> once daily
Oseltamivir
• Oral
• Bioavailabity: 80%, plasma protein binding low, t1/2 6-10 h, excretion
urine ( vs probenecid)

31
 Oseltamivir & Zanamivir (Cont’d)

Oseltamivir
• AEs: nausea, vomiting, abdominal pain

Zanamivir
• Inhaler
• PK: 10-20% reaches the lungs, t1/2 2,8 jam,
minimal metabolisme, urine excretion
• Aes: cough, bronchospasm, nasal throat discomfort

32
 Amantadine & Rimantadine
MoA
• Block the M2 proton ion channel of the virus particle and inhibit uncoating the
viral RNA within infected host celss

Used for
• Influenza A

PK
• Amantadine  well absorbed, 67% protein bound, t1/2 12-18 h, exc -> urine
(unchanged)
• Rimantadine  40% protein bound, t1/2 24-36 h, extensive metabolism before
urinary exc.

AEs
• GIT and CNS disturbance
33