LECCTURE OF PHARMACOLOGY

MADE BY NURSING ZONE TEAM

L5. Chemotheraputic agents II

THIRD YEAR

@Nursing_Zone39
 Antimycobacterium Antibiotics
Oral Rectal SC

Hmmmm
or Easy
A- Tuberclosis (TB)
or Verity
Mycobacteria: Bypasses
is a group of organisms, liverof diverse group of Patient
consist canbacteria.
acid-fast
orCompact
Erratic absorption low administer
Convenient
TB is caused by Mycobacterium tuberculosis, Complete
compliancewhich mainly problmatic because itcan
First pass effect
survive inside macrophages after phagocytosis. absorption
Sometimes inefficient
Small does
Treatment
difficultly in swallowing
Pain full
s1st line drugs: isoniazid, rifampicin, rifabutin, ethambutol andpyrazinamide.
Sublingual-Buccal IV streptomycin, clarithromycin
s2nd line drugs: capreomycin, cycloserine, IMand
ciprofloxacin.

TI Rapid absorption Rapid

Rifampicin drug I TI Large volume
E Stability of drug

GBBBEmMgm
Accurate
Action
Higher bioavailability
I K Sustained release
E Can’t
Bactericidal for mycobacteria. Also be retrieved
effective against most Gm+/-. Itinhibitspossible
bacterial (but not
Inconvenient
IX
human: selectivity) RNA polymerase. Resistance can develop rapidly, resulting from a chromosomal
XI Expensive Trained personnel
mutation.
Small doses only
EXRequires trained personnel Erratic absorption
sCan’t
Clinicalbeuse
swallowed

s1- TB (combination with other drug). s2- Leprosy.

s3- Prophylaxis for meningococcal meningitis. s 4- Haemophilus influenzae.
s5- Brucellosis. s 6- endocarditis legionnaires’ disease.
s 7- serious staphylococcus infections.

sAdverse effect
Best of luck

Skin Eruptions Fever GIT dist liver damage with jaundice

Fatal for few patients

e
So liver function should be
assessed before treatment
B- Leprosy
Oral Rectal SC

Hmmmm
Leprosy is Easy
or
Leprosy:
caused by the acid-fast bacillus: Mycobacterium leprae.

orisVerity
a chronic illness with along latency, and historically sufferers
Bypasses liver Patientforced
can to
or Compact
live away from their communities, although, in fact, the disease is not particularly
Erratic absorption low administer
Convenient
contagious.
compliance Complete
First pass effect
Treatment
absorption
s Sometimes
Paucibacillaryinefficient
leprosy: is treated for 6 months with dapsone+ rifampicin.
Small does
Multibacillary
sdifficultly leprosy: is treated for at least 2 years with rifampicin+dapsone+
in swallowing
clofazimine. Pain full

Sublingual-Buccal IV IM

TI Rapid absorption Antifungal

I RapidAntibiotics TI Large volume
E Stability of drug

GBBBEmMgm
Accurate
I K Sustained release
E Higher bioavailability
Difference
IX Can’t be retrieved
between Bacteria and Fungi
possible
XI Inconvenient Expensive Trained personnel
Small doses only
EXRequires trained personnel Erratic absorption
Can’t be swallowed
Bacteria Fungi

Have Nucleus (euokaryote)

Nucleus No Nucleus thus they are closer to human cell and
its metabolic pathways= less selectivity

Size Best of luck Small Bigger

Cell Single cells Multi-cellular

Shape Have 3 shapes Many shapes

Made of peptidoglycan
Cell wall Made of Chitin
(easier to target).
Clinical classification of fungi according to site of infection:
Oral Rectal SC

Hmmmm or Easy dermatophytes.

s 1-Cutaneous:
s 2-Systemic:
or VerityCoccidioides, Histoplasma.
s 3-Fungal
Patient can
Bypasses liver hosts (AIDS, corticosteroids
infections of immuno-compromised
Compact
or
Erratic absorption low
... cancer patients): Aspergillus. administer
Convenient
compliance Complete
First pass effect Pityriasis versicolor
s absorption
s Sometimes inefficient
Superficial
Small does
difficultly in swallowing s White piedra
Pain full

Sublingual-Buccal s Tinea pedisIV

(athlete’s foot) IM

TI Rapid absorption
Cutaneous Rapid
Onychomycosis (nail infection)
s
I s
TI Large volume
E Stability of drug

GBBBEmMgm
E Higher bioavailability
XI Inconvenient
Small doses only
Subcutaneous
s Can’t be swallowed
Accurate
I K Sustained release
IX Can’t be retrieved
s Tinea capitis (scalp ringworm) possible
Expensive Trained personnel
s Chromoblastomycosis
EXRequires trained personnel Erratic absorption
s Mycetoma

s Blastomycosis

s Histoplasmosis
s Systemic
Best of luck
s Coccidioidomycosis

s Paracoccidioidomycosis

s Candidosis

s Opportunistic s Aspergillosis

s Pneumonia
Drugs used to treat fungal infection
Oral Rectal SC

Hmmmm
s or Easy
Naturally occurring antifungals
or Verity
Bypasses liver
s Synthetic drugs
Patient can
sorA-polyenes
Compact sC-Azoles
Erratic absorption low administer
s B-echinocandin
Convenient sD-fluorinated pyrimidines
compliance Complete
First pass effect
absorption
Sometimes inefficient
Many antifungal agents are quite toxic, and when systemic therapy is
Small does
difficultly in swallowing
required these agents must often be used under strict medicalPain
supervision.
full

Sublingual-Buccal IV IM

TI Rapid absorption Rapid

I TI Large volume
E Stability of drug

GBBBEmMgm
Accurate
I K Sustained release
E Higher bioavailability
IX Can’t be retrieved possible
XI Inconvenient Expensive Trained personnel
Small doses only
EXRequires trained personnel Erratic absorption
Can’t be swallowed

Best of luck
 Antivirals
Oral Rectal SC

Hmmmmor Easy
Morphology of viruses
Verity
or
Bypasses liver Patient can
or Compact
‫ اﳊﺒﻮب اﻟﻠﻲ ﺗﻄﻠﻊ ﰲ اﻟﺸﻔﺎﻳﻒ واﳋﺸﻢ واﻟﻌﲔ ﺗﻜﻮن ﻣﻌﺪﻳﺔ‬Erratic
‫اﻟﺸﺎﺋﻊ‬absorption
‫ اﻟﻨﻮع‬s low administer
Convenient
compliance ‫ ﻓﻴﻬﺎ‬Complete
‫ﻳﺼﻴﺐ اﻟﻐﺪة اﻟﻨﻜﺎﻓﻴﺔ وﻳﺴﺒﺐ ورم‬
First pass effect
absorption
Sometimes inefficient
‫ﻫﺬا اﻟﻨﻮع ﻳﺼﻴﺐ اﻟﻨﺒﺎﺗﺎت‬ Small does
difficultly in swallowing
Pain full

Sublingual-Buccal IV IM

TI Rapid absorption Rapid

I TI Large volume
E Stability of drug

GBBBEmMgm
Accurate ‫داء اﻟﻜﻠﺐ‬
I K Sustained release
E Higher bioavailability
IX Can’t be retrieved possible
XI Inconvenient Expensive Trained personnel
Small doses only
‫اﻟﻐﺪد‬Requires
‫ﻣﺜﻞ اﻟﻠﻮز وﻳﺼﻴﺐ اﳉﻬﺎز اﻟﺘﻨﻔﺴﻲ‬EX ‫ﻳﺼﻴﺐ‬ trained personnel Erratic absorption
Can’t be swallowed ‫ﺷﻠﻞ اﻻﻃﻔﺎل‬

Properities of viruses
Best of luck
s 1- Size (smaller than bacteria)

s 2- Nucleic acid content (DNA/RNA: Viruses are not cells): Viruses contain only
a singl type of nucleic acid: either DNA or RNA.

s 3- Metabolic capabilities (obligatory intracellular parasites)

 Antiviral drugs
Oral Rectal SC

Hmmmm
Selectivity is the main issue, as virus enters host cell and capture its

Most
or Easyprocess for itself. The solution is: Targeting virus-specific enzymes.
metabolic
Verity
or of antivirals are effective during replication only.
Bypasses liver Patient can
or Compact
Erratic absorption low administer
Convenient
compliance Complete
First pass effect
absorption
Sometimes inefficient
Small does
difficultly in swallowing
Pain full

Sublingual-Buccal IV IM

TI Rapid absorption Rapid

I TI Large volume
E Stability of drug

GBBBEmMgm
Accurate
I K Sustained release
E Higher bioavailability
IX Can’t be retrieved possible
XI Inconvenient Expensive Trained personnel
Small doses only
EXRequires trained personnel Erratic absorption
Can’t be swallowed

Best of luck
 Immuno-pharmacology
Oral Rectal SC

Hmmmm or Easy
Interferon-alpha
or Verity
IFN-α
Bypasses liver Patient can
or Compact
Action Erratic absorption low administer
Convenient
compliance Complete
First
Killspass effect
viruses and virus infected cells. They have a broad spectrumof action
s absorption
Sometimes inefficient
and inhibit the replication of most viruses in vitro
Small does
difficultly in swallowing
Pain full
s MoA
Sublingual-Buccal IV IM
sIt stimulates the production of host enzymes that degrade both viral mRNA
TI Rapid
(thus absorption
inhibiting viral protein synthesis and halting replication) and host cell
Rapid it.
mRNA in the infected cell, thus I killing TI Large volume
E Stability of drug

GBBBEmMgm
Accurate
I K Sustained release
E Higher bioavailability
s Abs/Distrb/Elim
Inconvenient
IX Can’t be retrieved possible
XI Expensive Trained personnel
Small
Give doses
IV, T only
½ 2-4h. IM: peak blood conc. are reached in 5-8h. They do not cross
s
EXRequires trained personnel Erratic absorption
Can’t
the be swallowedbarrier. Peginterferon-alfa2a has a longer T ½.
blood-brain

s Clinical use

s For viral hepatitis B.

s With ribavirin for chronic viral hepatitis C.

Best of luck
s Adverse effects

s Fever, headached and myalgia are common.

s CVS and liver dysfunction and bone marrow depression can occur.
 Anti-helminthic drugs
Oral Rectal SC

Hmmmm
s
or Easy
Major groups of helminths
or Verity
Bypasses liver Patient can
or Compact
v v
Erratic absorption low administer
v
Convenient
Nematodes Trematodes Cestodes
compliance Complete
First pass effect
s Diethylcarbamazine s Praziquantel absorption
s Albendazole
Sometimes
s Ivermectininefficient s Niclosamide
Small does
s Mebendazole
difficultly in swallowing
s Pyrantel pamoate Pain full
s Thiabendazole
Sublingual-Buccal IV IM
Benzimidazole (Thiabendazole, Albendazole and Mebendazole)
s
TI Rapid absorption
I Rapid
Effective against wide spectrum of nematodes
Stability of drug
TI Large volume

GBBBEmMgm
E
Higher
Action bioavailability
and Mechanism of
I Accurate
action K Sustained release
Es
Inconvenient
IX Can’t be retrieved possible
XIs It acts by binding and interfering Expensive Trained personnel
the assembly of microtubules.
Small doses only
EXRequires trained personnel Erratic absorption
Can’t be swallowed
s Pharmacokinetics of Benzimidazole

s Poorly absorbed from GIT except if given with fatty meals.

s Clinical use
Best of luck
s For intestinal nematode infections.

s Adverse effects

s Albendazole and Mebendazole are well tolerated.

s Thiabendazole causes hallucinations.

Contraindicate in pregnancy
 Anti-protozoal drugs
Oral Rectal SC

Hmmmm
s
or Easy
Groups of Anti-protozoal drugs
or Verity
Bypasses liver Patient can
or Compact
Erratic absorption administer
Convenient
Amebiasis Malaria low Trypanosomiasis
s
compliance Complete
First pass effect
sChloroquine s Artemisinin absorption
s Benznidazole
Sometimes inefficient
s Dehydroemetine s Chloroquine s Melarsoprol
Emetine Small does
difficultly
s in swallowing s Mefloquine s Nifurtimox
s lodoquinol s Primaquine Pain full
s Pentamidine
s Metronidazole s Pyrimethamine s Suramin
Sublingual-Buccal
s Paramomycin IV
s Quinine/Quinidine IM
s Tinidazole

TI Rapid absorption Rapid

Leishmaniasis I Toxoplasmosis TI LargeGiardiasis
volume
E Stability of drug

GBBBEmMgm
s
Accurate
I Pyrimethamine K Sustained release
E sHigher
Sodium bioavailability
stibogluconate Metronidazole
IX Can’t be retrieved
s s
possible
s Nitazoxanide
XI Inconvenient Expensive Trained personnel
s Tinidazole
Small doses only
EXRequires trained personnel Erratic absorption
s Can’t be swallowed
Metronidazole

s Mechanism of action Pharmacokinetics of Benzimidazole

s

s Damaging the protozoa DNA. s Widely distributed in the body

Best of luck
Kill e
secretions– semen, vagina, saliva
and CSF

s Clinical use s Adverse effects

s Ameobiasis; Giardiasis; Trichomonas s Nausea

vaginalis (both partners). s Metallic taste
s Anaerobic infections: Helicobacter pylori
 Chloroquine
Oral Rectal SC

Hmmmm
s or Easy
Mode of
or Verity
action

Blood schizonticides Bypasses liver Patient can

or Compact
s
Erratic absorption low administer
Convenient
compliance Complete
s First pass effect
Pharmacokinetics of Benzimidazole
absorption
Sometimes inefficient
s Oral & parenteral {slow infusion or IM} Small does
difficultly in swallowing
s Crosses the placenta Pain full

Sublingual-Buccal IV IM
s Clinical use
TI Rapid absorption
Usedof
Stability todrug I Rapidvivax, P. ovale, P. malariae,
treat malaria: Plasmodium TI Large and
volume

GBBBEmMgm
E s
Higher
I Accurate
sensitive strains of. P. falciparum.
bioavailability K Sustained release
E
IX Can’t
s Chemoprophylaxis: against
Inconvenient
allbe retrieved
forms possible
of malaria {except Chloriquine-
XI resistant P. falciparum} Expensive Trained personnel
Small doses only
EXRequires trained personnel Erratic absorption
Can’t be swallowed
Adverse effects
s

s GIT symptoms
s Anorexia
s Headache
s Pruritus
Best of luck
s Blurred vision
s Cardiac depressant effect

Contraindicate in pregnancy
 Anticancer drugs
Oral Rectal SC

Hmmmm or Easy
or Verity
Definition
Bypasses liver Patient can
or Compact
s Uncontrolled multiplicationErratic absorption
and spread low
of abnormal forms ofadminister
cells=
Convenient
craziness of the cells (‫)ﺟﻨﻮن اﳋﻠﻴﺔ‬compliance Complete
First pass effect
s Cancer (new growth)= tumour = neoplasm= malignancy absorption
Sometimes inefficient
s All multicellular organisms can be afflicted by cancer Small does
difficultly in swallowing
Pain full
Causes of cancer
s Sublingual-Buccal IV IM

s Rapid
TI absorption
Genetic disease s Chemical carcinogen and radioactive materials.
Rapid
I TILarge volume
E Stability of drug

GBBBEmMgm
Accurate
I K Sustained release
EsHigher bioavailability
Environmental exposure. ex: UV radiation
IX Can’t be retrieved possible
XI Inconvenient Expensive Trained personnel
Small doses only
EXRequires
Hallmarks (Characteristics) trained personnel
of cancer Erratic absorption
s Can’t be swallowed

s Uncontrolled proliferation s Invasiveness

s Dedifferentiation and loss of function Metastasis

s

Best of luck
s Apoptosis

s Apoptosis is the programmed cell death (for all cells), by whichbody remove
cells (favourable: apoptosis and apoptotic gens).
 Summary of the main targets for anticancer drug therapy
Oral Rectal SC

Hmmmm or Easy
or Verity
Bypasses liver Patient can
or Compact
Erratic absorption low administer
Convenient
compliance Complete
First pass effect
absorption
Sometimes inefficient
Small does
difficultly in swallowing
Pain full

Sublingual-Buccal IV IM

TI Rapid absorption Rapid

I TI Large volume
E Stability of drug

GBBBEmMgm
Accurate
I K Sustained release
E Higher bioavailability
IX Can’t be retrieved possible
XI Inconvenient Expensive Trained personnel
s Alkylating agents
Small doses only
EXRequires trained personnel Erratic absorption
Can’t be swallowed
s Bifunctional alkylating agents A can cause in DNA

Intrastrand linking e Cross-linking e

s Best of luck
Mustard Gas was first used by the German army in worldwarI (stronglylethal).

s British soldiers blinded by mustard gas

Treatment
Oral Rectal SC

Hmmmm
s
or Easy
Radioactive
or Verity
isotopes
Bypasses liver Patient can
or sCompact
Important for certain tumours: e.g. radioactive iodine
Erratic absorption low administer
Convenient
compliance
Thyroid tumours e Complete
First pass effect
absorption
Sometimes inefficient
Small does
difficultly in swallowing
Pain full
s Monoclonal antibodies (Trastuzumab (Herceptin))
Sublingual-Buccal IV IM
s Binds to a protein termed HER2 (tyrosine kinase receptor)

TI Rapid absorption for treatment ofRapid

breast cancer
I TI Large volume
E Stability of drug
e

GBBBEmMgm
Accurate
I K Sustained release
E Higher bioavailability
Inconvenient
IX Can’t be retrieved possible
s Protein kinase inhibitors (Imatinib)
XI Expensive Trained personnel
Small doses only
EXRequires trained personnel Erratic absorption
Can’t be swallowed
Action and MoA
s

s Inhibits protein kinases

s Clinical use

Best of luck
s Chronic myeloid leukaemia
s Acute lymphoblastic leukemia
Some GIT tumours which are not susceptible to surgery
s

s Adverse effects

sGIT symptoms (pain, diarrhoea, nausea) s Fatigue

sPhotosensitivity s Headaches
s Sometimes rashes.
MADE BY NURSING ZONE TEAM

Pharma references

A- Basic and Clinical Pharmacology 13 E Paperback

Bertram Katzung (Author), Anthony Trevor (Author) Publisher: McGraw-Hill Medical; 13 edition
(December 23, 2014)
Language: English
ISBN13:97 0071825054
ISBN 10:0071825053
B. Lippincott Illustrated Reviews: Pharmacology 6th edition (Lippincott Illustrated Reviews Series)
Paperback
Karen Whalen PharmD BCPS (Author) Edition: Sixth, North American.
Edition Language: English. ISBN-13: 978-1451191776 ISBN-10: 1451191774
2. List Essential References Materials (Journals, Reports, etc.) British National Formulary (BNF)