‫بسم هللا الرحمن الرحيم‬

‫‪1‬‬
 Chemotherapy
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Tetracyclines

Dr. Asmaa Fawzy

Pharmacology Department
Tanta university
Contact/ 01069625853
 Objectives (ILOs)

Upon completion of this lesson, the student will be able to:

Discuss different pharmacological aspects of
Tetracyclines including:

➢ Pharmacokinetics
➢ Pharmacodynamics
➢ Uses
➢ Adverse effects
➢ Drug interactions
Remember,….

Classification of antimicrobials

1- According to type of organism:

• Antibacterial, antiviral,
• Antifungal, antiprotozoal,
Anthelmintics.

Antibacterial drugs can be subdivided into:

• Bacteriostatic
• Bactericidal
• Both
Antibacterial drugs
Where Antimicrobials work?
 2. According to Mechanism of action

Inhibition of
Inhibition of cell Inhibition of Inhibition of Nucleic Folic Acid
wall synthesis protein synthesis Acid Synthesis Synthesis

✓Penicillins ✓Macrolides ✓Quinolones ✓Sulfonamides

✓Cephalosphorins ✓Aminoglycosides
✓Rifampin ✓Trimethoprim
✓Carbopenems ✓Amphenicols
✓Monobactams
✓Tetracyclines
✓Vancomycin
About any antibiotic, you should know….:

➢ Classification / Chemistry
➢ Kinetics
➢ Dynamics (Mechanism of action)
➢ Spectrum (esp. exception)
➢ Uses
➢ Side effects
➢ Contraindications
➢ Drug interactions
Tetracyclines
Classification

Low to moderate High

lipid solubility lipid solubility

Tetracycline Doxycycline

oxytetracycline Minocycline
 Pharmacokinetics:

Low – moderate High

lipid solubility lipid solubility

Absorption Incomplete Complete

Affected by meal → Milk, Ca+2, Mg+2 & Al+3 →

↓ tetracycline absorption: (non-absorbable chelate).

All over body, pass BBB & placental barrier. ???

Distribution
Concentrated at calcification sites (bone & teeth). ???
 Low – moderate High
lipid solubility lipid solubility

Metabolism Hepatic metabolism.

Excretion ▪ Mainly in urine by ▪ Doxycycline → in feces

passive filtration. (allowed in renal
patients).
▪ Bile → pass in stool or
undergoes enterohepatic
circulation. ▪ Minocycline → urine,
feces, milk, tears & saliva.
▪ Milk.
* Minocycline also achieves high levels in

saliva and tears, rendering it useful in

eradicating the meningococcal carrier state.

* Doxycycline is preferred in casas of renal

impairment, as it is eliminated through the
bile into the feces.
 Dynamics
• Broad spectrum bacteriostatic antibiotics.

• Bind to 30s ribosomal subunits leading to inhibition of

protein synthesis.
 Uses
• Gram +ve & -ve bacterial infection (Not TB + Typhoid):
– Respiratory & E.N.T. infection, drug of CHOICE in mycoplasma
pneumonia.

– Minocycline → Meningococcal carrier.

– Cholera (Doxycycline ), Bacillary dysentery (Shigella &

Salmonella)

– Urinary tract infection (UTI)

– Acne vulgaris

– Eye infection
• Rickettsia infection.

• Chlamydia infection.

➢ Demeclocycline: (it interferes with ADH release).

Used in TTT of Syndrome of Inappropriate ADH secretion

(SIADH) = Too much antidiuretic hormone (ADH).

Side effects
of Tetracyclines
 Side effects
• Teeth & Bone abnormalities:
- Teeth → Permanent yellow-brown discoloration, deformity.
- Bone → deformity & inhibit bone growth.

=> Tetracyclines should be avoided during pregnancy, lactation

& in children up to 8 years, why?
• GIT irritation,
• Inhibit intestinal flora,

• Hepatotoxicity,
• Nephrotoxicity,

• Hypersensitivity ,
• Photosensitivity.
➢ Minocycline: causes benign increase in intracranial
pressure (Pseudo-tumor cerebri) as it passes CNS.

➢ Demeclocycline: Diabetes insipidus like syndrome;

(anti-ADH), (interfere with ADH release).

- Diabetes mellitus is caused by your

body being unable to produce the
insulin it needs.
- Diabetes insipidus is a disease where
kidneys are unable to conserve water.
Assess yourself
!!!
1. A tetracycline antibiotic that is used for eradication of
the meningococcal carrier state:
a. Demeclocycline
b. Minocycline
c. Oxytetracycline
d. Doxycycline

1. A tetracycline antibiotic that is used for eradication of the

meningococcal carrier state:
a. Demeclocycline
b. Minocycline
c. Oxytetracycline
d. Doxycycline
3. A tetracycline antibiotic that is allowed in renal patients because
of its biliary excretion:
a) Doxycycline
b) Minocycline
c) Oxytetracycline
d) Amoxicillin

3. A tetracycline antibiotic that is allowed in renal patients because

of its biliary excretion:
a) Doxycycline
b) Minocycline
c) Oxytetracycline
d) Amoxicillin
4. A tetracycline antibiotic that is allowed in treatment of
syndrome of inappropriate ADH secretion:
a) Demeclocycline
b) Minocycline
c) Oxytetracycline
d) Amoxacillin

4. A tetracycline antibiotic that is allowed in treatment of

syndrome of inappropriate ADH secretion:
a) Demeclocycline
b) Minocycline
c) Oxytetracycline
d) Amoxacillin
5. Minocycline is highly useful in eradicating the meningococcal
carrier state for which one of the following causes?

a. It is concentrated in the cerebrospinal fluid

b. It achieves high levels in saliva and tears

c. It has no major CNS adverse effects

d. It is a broad spectrum bactericidal

5. Minocycline is highly useful in eradicating the meningococcal

carrier state for which one of the following causes?
a. It is concentrated in the cerebrospinal fluid
b. It achieves high levels in saliva and tears
c. It has no major CNS adverse effects
d. It is a broad spectrum bactericidal