DRUGS USED FOR THE DRUGS USED FOR THE TREATMENT OF SYPHILISTREATMENT OF SYPHILIS & GONORRHEA & GONORRHEA

Prof. Mohammad AlhumayydProf. Mohammad Alhumayyd

OBJECTIVESOBJECTIVES

At the end of lecture , the At the end of lecture , the students should understand:students should understand:

The drugs used in the The drugs used in the treatment of syphilis & treatment of syphilis & gonorrhea.gonorrhea.

The mechanism of action, The mechanism of action, adverse effects of each drug adverse effects of each drug

OBJECTIVES ( continue)OBJECTIVES ( continue)

The contraindications of drugs The contraindications of drugs used used

The recommended regimens The recommended regimens used for treatment of syphilis & used for treatment of syphilis & gonorrhaeagonorrhaea

The alternative treatments in The alternative treatments in allergic patientsallergic patients

SYPHILIS SYPHILIS

What is Syphilis?What is Syphilis?Sexually transmitted Sexually transmitted disease caused by disease caused by bacterium bacterium TreponemaTreponema PallidumPallidum

Stages Of SyphilisStages Of Syphilis

A primary stage ( a single A primary stage ( a single sore ( a chancre ) )sore ( a chancre ) )

Secondary StageSecondary Stage

Skin rash & mucous Skin rash & mucous membranes lesionsmembranes lesions

Latent stageLatent stage

70% may have NO SYMPTOMS70% may have NO SYMPTOMS

Drugs used in the treatment Drugs used in the treatment of Syphilisof Syphilis PenicillinsPenicillins******

Penicillin GPenicillin G

Benzathin P. ; Procaine P.Benzathin P. ; Procaine P. TetracyclinesTetracyclines

DoxycyclineDoxycycline MacrolidesMacrolides

ClarithromycinClarithromycin CephalosporinsCephalosporins

CeftriaxoneCeftriaxone

PENICILLINSPENICILLINS

Mechanism of actionMechanism of action Inhibit the synthesis of Inhibit the synthesis of

bacterial cell wall .bacterial cell wall .

These drugs are These drugs are bactericidalbactericidal

Preparations of penicillins used Preparations of penicillins used for the treatment of syphilisfor the treatment of syphilis

Penicillin GPenicillin G, , i.vi.v(Short duration of action(Short duration of action) Procaine P,i.m Procaine P,i.m (Long acting(24-48hrs)(Long acting(24-48hrs)

Benzathine P,i.mBenzathine P,i.m(Long acting(every 3-4(Long acting(every 3-4

weeks) weeks)

All are:All are:

Acid unstableAcid unstable Penicillinase sensitivePenicillinase sensitive

Adverse effects of Adverse effects of penicillinspenicillins

HypersensitivityHypersensitivity Convulsions with high Convulsions with high

doses or in renal failuredoses or in renal failure Super infectionsSuper infections

Drugs used in Allergic PatientsDrugs used in Allergic Patients To Penicillins To Penicillins

Tetracyclines such as:Tetracyclines such as:DoxycyclineDoxycycline

MacrolidesMacrolides such assuch as::Clarithromycin Clarithromycin

Cephalosprins such as :Cephalosprins such as :CeftriaxoneCeftriaxone

cefiximecefixime

TETRACYCLINESTETRACYCLINES

e.g, Doxycyclinee.g, Doxycycline

Well absorbed orally Well absorbed orally Long-acting Long-acting

Mechanism of action Mechanism of action

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

Side effectsSide effects

1. nausea, vomiting ,diarrhea & 1. nausea, vomiting ,diarrhea & epigastric pain(give with food)epigastric pain(give with food)

2. Hepatic toxicity ( prolonged 2. Hepatic toxicity ( prolonged therapy with high dose )therapy with high dose )

3. Brown discolouration of teeth 3. Brown discolouration of teeth – children– children

4. Deformity or growth 4. Deformity or growth inhibition of bones – childreninhibition of bones – children

5. Vertigo 5. Vertigo 6. Superinfections. 6. Superinfections.

ContraindicationsContraindications

PregnancyPregnancy

Breast feedingBreast feeding

Children(below 10 yrs)Children(below 10 yrs)

1717

MACROLIDES MACROLIDES e.g., clarithromycin e.g., clarithromycin

Mechanism of action Mechanism of action

Inhibits bacterial protein Inhibits bacterial protein synthesis by binding to synthesis by binding to bacterial 50S ribosomal bacterial 50S ribosomal subunitssubunits

Side EffectsSide Effects

Nausea, vomiting, abdominal pain Nausea, vomiting, abdominal pain & diarrhea.& diarrhea.

Allergic reactions- urticaria, mild Allergic reactions- urticaria, mild skin rashesskin rashes

Irregular heart beats(recent)Irregular heart beats(recent)

Cephalosporins

β-lactam antibiotics

3rd Generation cephalosporins

e.g. Ceftriaxone

cefixime

Mechanism of action

Inhibits bacterial cell wall synthesis

Bactericidal

Adverse effectsAdverse effects

Allergic manifestationsAllergic manifestations

ThrombophilibitisThrombophilibitis

SuperinfectionSuperinfection

DiarrheaDiarrhea

GONORRHEAGONORRHEA

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 Drugs used in the treatment of Gonorrheaof Gonorrhea

33rdrd generation Cephalosporins generation Cephalosporins******

Ceftriaxone,I.M, Cefixime,P.OCeftriaxone,I.M, Cefixime,P.O FluoroquinolonesFluoroquinolones

CiprofloxacinCiprofloxacin SpectinomycinSpectinomycin

::Recommended regimensRecommended regimens ( 1( 1stst line treatment) line treatment)

Uncomplicated gonorrheal Uncomplicated gonorrheal

infectionsinfections

33rdrd generation cephalosporinsgeneration cephalosporins

500mg ceftriaxone,IM 500mg ceftriaxone,IM

or 400 mg of cefixime,poor 400 mg of cefixime,po

Typically given with a single dose Typically given with a single dose

of azithromycin(1gm,po) orof azithromycin(1gm,po) or

doxycycline(100mg,b.i.d,po) for 7 doxycycline(100mg,b.i.d,po) for 7

days.days.

FLUOROQUINOLONESFLUOROQUINOLONES

Single oral dose of :Single oral dose of :

Ciprofloxacin(500 mg) Ciprofloxacin(500 mg)

Ofloxacin(400 mg)Ofloxacin(400 mg)

MECHANISM OF ACTION of MECHANISM OF ACTION of fluoroquinolonesfluoroquinolones

All are bactericidalAll are bactericidal

Inhibit DNA synthesis by Inhibit DNA synthesis by inhibiting DNA gyrase enzymeinhibiting DNA gyrase enzyme

Side effectsSide effects

Nausea , vomiting & diarrhoeaNausea , vomiting & diarrhoeaHeadache & dizziness Headache & dizziness May damage growing cartilage May damage growing cartilage

&cause arthropathy.&cause arthropathy.Phototoxicity – avoid excessive Phototoxicity – avoid excessive

sunlightsunlight

CONTRAINDICATIONSCONTRAINDICATIONS

PregnancyPregnancy

Nursing mothersNursing mothers

Children under 18 yearsChildren under 18 years

Alternative treatment in pts cannot Alternative treatment in pts cannot tolerate or be treated with 1 tolerate or be treated with 1stst line line treatmenttreatment

SpectinomycinSpectinomycin

2g ,IM2g ,IM

Mechanism of actionMechanism of action

Inhibits protein synthesis Inhibits protein synthesis by binding to 30 S by binding to 30 S ribosomal subunitsribosomal subunits

1. Pain at the site of injection

Adverse Effects

Nephrotoxicity

(not common)

2. Fever

Nausea

CONTINUECONTINUE

CComplicated gonorrheal omplicated gonorrheal infectionsinfections

Spread through blood streamSpread through blood stream EYEEYE JointsJoints Heart valvesHeart valves BrainBrain

Harmful effects of gonorrheaHarmful effects of gonorrhea

Newborn eye infections, may lead to blindness

Treatment of Complicated Treatment of Complicated infections infections

With With conjunctivitisconjunctivitis in new in new bornborn

Silver nitrateSilver nitrate

GermicidalGermicidal effects are due effects are due to precipitation of bacterial to precipitation of bacterial proteins by liberated silver proteins by liberated silver ionsions

Silver nitrate ( continue)Silver nitrate ( continue)

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

ERYTHROMYCINERYTHROMYCIN

0.5% ointement for teatment 0.5% ointement for teatment & prevention of corneal & & prevention of corneal & conjunctival infections.conjunctival infections.

Put into conjunctival sac Put into conjunctival sac immediately after birth (no immediately after birth (no later than 1 hr after delivery )later than 1 hr after delivery )