DRUGS USED FOR THE TREATMENT OF SYPHILIS & GONORRHEA

Prof. Mohammad Alhumayyd

OBJECTIVES OBJECTIVES At the end of lecture, the students should understand: At the end of lecture, the students should understand: The drugs used in the treatment of syphilis & gonorrhea. The drugs used in the treatment of syphilis & gonorrhea. The mechanism of action, adverse effects of each drug The mechanism of action, adverse effects of each drug

OBJECTIVES ( continue) The contraindications of drugs used The contraindications of drugs used The recommended regimens used for treatment of syphilis & gonorrhaea The recommended regimens used for treatment of syphilis & gonorrhaea The alternative treatments in allergic patients The alternative treatments in allergic patients

SYPHILIS SYPHILIS What is Syphilis? Sexually transmitted disease caused by bacterium Treponema Pallidum Sexually transmitted disease caused by bacterium Treponema Pallidum

Stages Of Syphilis A primary stage ( a single sore ( a chancre ) ) A primary stage ( a single sore ( a chancre ) )

Secondary Stage Skin rash & mucous membranes lesions Skin rash & mucous membranes lesions

Latent stage 70% may have NO SYMPTOMS

Drugs used in the treatment of Syphilis Penicillins*** Penicillins*** Penicillin G Penicillin G Benzathin P. ; Procaine P. Benzathin P. ; Procaine P. Tetracyclines Tetracyclines Doxycycline Doxycycline Macrolides Macrolides Clarithromycin Clarithromycin Cephalosporins Cephalosporins Ceftriaxone Ceftriaxone

PENICILLINS PENICILLINS Mechanism of action Mechanism of action Inhibit the synthesis of bacterial cell wall. Inhibit the synthesis of bacterial cell wall. These drugs are bactericidal These drugs are bactericidal

Preparations of penicillins used for the treatment of syphilis Penicillin G, i.v (Short duration of action Penicillin G, i.v (Short duration of action ) Procaine P,i.m (Long acting(24-48hrs) Procaine P,i.m (Long acting(24-48hrs) Benzathine P,i.m (Long acting(every 3-4 Benzathine P,i.m (Long acting(every 3-4 weeks) weeks) All are: All are: Acid unstable Acid unstable Penicillinase sensitive Penicillinase sensitive

Adverse effects of penicillins Hypersensitivity Hypersensitivity Convulsions with high doses or in renal failure Convulsions with high doses or in renal failure Super infections Super infections

Drugs used in Allergic Patients To Penicillins Drugs used in Allergic Patients To Penicillins Tetracyclines such as: Tetracyclines such as:Doxycycline Macrolides such as: Macrolides such as:Clarithromycin Cephalosprins such as : Cephalosprins such as :Ceftriaxone cefixime cefixime

TETRACYCLINES e.g, Doxycycline e.g, Doxycycline Well absorbed orally Well absorbed orally Long-acting Long-acting

Mechanism of action Inhibit bacterial protein synthesis by reversibly binding to 30 S bacterial ribosomal subunits. Inhibit bacterial protein synthesis by reversibly binding to 30 S bacterial ribosomal subunits.

Side effects 1. nausea, vomiting,diarrhea & epigastric pain(give with food) 2. Hepatic toxicity ( prolonged therapy with high dose ) 3. Brown discolouration of teeth – children 4. Deformity or growth inhibition of bones – children 5. Vertigo 6. Superinfections.

Contraindications Pregnancy Pregnancy Breast feeding Breast feeding Children(below 10 yrs) Children(below 10 yrs) 17

MACROLIDES e.g., clarithromycin Mechanism of action Mechanism of action Inhibits bacterial protein synthesis by binding to bacterial 50S ribosomal subunits Inhibits bacterial protein synthesis by binding to bacterial 50S ribosomal subunits

Side Effects Nausea, vomiting, abdominal pain & diarrhea. Allergic reactions- urticaria, mild skin rashes Irregular heart beats(recent)

Cephalosporins β-lactam antibiotics 3 rd Generation cephalosporins e.g. Ceftriaxone cefixime Mechanism of action Inhibits bacterial cell wall synthesis Bactericidal

Adverse effects Allergic manifestations Allergic manifestations Thrombophilibitis Thrombophilibitis Superinfection Superinfection Diarrhea Diarrhea

GONORRHEA Caused by Neisseria gonorrhea, a pus producing bacteria Up to 1 MILLION people affected each year Teenagers (15-19) have the highest rate if infection

Drugs used in the treatment of Gonorrhea 3 rd generation Cephalosporins*** 3 rd generation Cephalosporins*** Ceftriaxone,I.M, Cefixime,P.O Ceftriaxone,I.M, Cefixime,P.O Fluoroquinolones Fluoroquinolones Ciprofloxacin Ciprofloxacin Spectinomycin Spectinomycin

:Recommended regimens ( 1 st line treatment) :Recommended regimens ( 1 st line treatment) Uncomplicated gonorrheal Uncomplicated gonorrheal infections infections 3 rd generation cephalosporins 3 rd generation cephalosporins 500mg ceftriaxone,IM 500mg ceftriaxone,IM or 400 mg of cefixime,po or 400 mg of cefixime,po Typically given with a single dose Typically given with a single dose of azithromycin(1gm,po) or of azithromycin(1gm,po) or doxycycline(100mg,b.i.d,po) for 7 doxycycline(100mg,b.i.d,po) for 7 days. days.

FLUOROQUINOLONES FLUOROQUINOLONES Single oral dose of : Ciprofloxacin(500 mg) Ciprofloxacin(500 mg) Ofloxacin(400 mg) Ofloxacin(400 mg)

MECHANISM OF ACTION of fluoroquinolones All are bactericidal All are bactericidal Inhibit DNA synthesis by inhibiting DNA gyrase enzyme Inhibit DNA synthesis by inhibiting DNA gyrase enzyme

Side effects Nausea, vomiting & diarrhoea Headache & dizziness May damage growing cartilage &cause arthropathy. Phototoxicity – avoid excessive sunlight

CONTRAINDICATIONS Pregnancy Pregnancy Nursing mothers Nursing mothers Children under 18 years Children under 18 years

Alternative treatment in pts cannot tolerate or be treated with 1 st line treatment Spectinomycin 2g,IM 2g,IM

Mechanism of action Inhibits protein synthesis by binding to 30 S ribosomal subunits Inhibits protein synthesis by binding to 30 S ribosomal subunits

1.Pain at the site of injection Adverse Effects Nephrotoxicity (not common) 2. Fever Nausea

CONTINUE Complicated gonorrheal infections Complicated gonorrheal infections Spread through blood stream  EYE Joints Joints Heart valves Heart valves Brain Brain

Harmful effects of gonorrhea Newborn eye infections, may lead to blindness

Treatment of Complicated infections With conjunctivitis in new born With conjunctivitis in new born Silver nitrate Silver nitrate Germicidal effects are due to precipitation of bacterial proteins by liberated silver ions

Silver nitrate ( continue) Put into conjunctival sac once immediately after birth (no later than 1 h after birth ) Put into conjunctival sac once immediately after birth (no later than 1 h after birth )

ERYTHROMYCIN 0.5% ointement for teatment & prevention of corneal & conjunctival infections. 0.5% ointement for teatment & prevention of corneal & conjunctival infections. Put into conjunctival sac immediately after birth (no later than 1 hr after delivery ) Put into conjunctival sac immediately after birth (no later than 1 hr after delivery )