drugs used for the treatment of syphilis & gonorrhea
TRANSCRIPT
DRUGS USED FOR THE DRUGS USED FOR THE TREATMENT OF SYPHILISTREATMENT OF SYPHILIS & GONORRHEA & GONORRHEA
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
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
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 )