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DRUGS ACTING ON UTERUS AND ERECTILE DYSFUNCTION

UTERINE STIMULANTS
1. oxytoxin
 Physiological action :
 Milk ejection
 Increase force and frequency of uterine contraction
 Weak ADH activity
 VC
 Clinical indications :
IV infusion
Intra-nasal
 Induce and reinforce of oxytoxin
 Impaired milk
ejection
 Condition require early vaginal
deliveries (maternal DM, preeclampsia)
 Uterine inertia
 Incomplete abortion
 Control postpartum and post-abortal uterine
hemorrhage
 Adverse effect :
 Hypertension
 Uterine rupture
2. ergonovine – ergot alkaloid
 Effects :
- powerful stimulation of uterus contraction to
a. alpha-1 receptor agonist
b. 5-HT receptor agonist (serotonin)
- VC
 Clinical used :
 IM to reduce postpartum bleeding and should be given after
delivery of placenta
 Adverse effect ;
 Vomiting
 Hypertension
 Blurred vision
 Headache
 Angina

TOCOLYTIC THERAPY

indication :
inhibit uterine
contraction
postpone delivery in
cases of pretern
labor (before 37
weeks of gestation)
prolong pregnancy
from 48hrs – 1 week
provide sufficient
time for
administration for
antenatal
glucocorticoid helps
in fetal lung
maturation and
reduce neonatal
respiratory distress
contraindication :
intra-uterine
infection
fetal distress
vaginal bleeding
drug used ;

1. magnesium sulphate
- antagonizes IC calcium in
uterine ms  sm ms
relaxation
- given IV infusion

ERECTILE DYSFUNCTION
1. first line therapy
A. Oral VD
 Drugs : PDE5 inhibitors
sildenafil
vardenil
tadalafil
 Mode of action :
1. sexual arousal  release NO from NANC +
endothelial cell  activation of guanyl cyclase
 convert GTP to cGMP  sm ms relaxation 
VD of penile arteries and cavernosal spaces 
erection
2. sildenafil inhibit PDE5  increase catabolism
of cGMP  maintain VD and erection 
enhanced sexual performance
 Pharmacokinetic :
Sildenafil + virdenafil = peak 1hr & half
life of 4-5hrs
Take in empty stomach and to time
sexual activity so that it occurs within
1-6hrs
Tadalafil peak occurs 2hrs and half life
of approximately 18hrs
Erection function continues to be
enhanced for at least 36hrs
 Unwanted effects :
Hypotension
Flushing
Headache
Visual disturbances
Contraindicated with NO (
nitroglycerine, isosorbide
mononitrates, isosorbide dinitrate)

3. prostaglandins
 Pharmacological effect on uterus :
 PGF2-alpha, PGE1 and PGE2 produce coordinated contraction
of the body of pregnant uterus and relax cervix
 Clinical use :
Induction of abortion
Induction of labor
 Terminate pregnancy at 1s and
nd
2 trimester
 DINOPROSTONE
 DINOPROSTONE
 Available as vaginal insert, gel
and suppositories
 Given by vaginal administration
 MISOPROSTOL
 Orally combined with
mifepristone (antiprogestin)
 Adverse effect:
Nausea
vomiting

2. dihydropyridine CCB ;
Nifedipine
- block calcium channels and
decrease calcium entry into
uterine sm ms with
subsequent relaxation
- given sublingually every 1520 min for doses then given
oral every 406hrs
3. beta adrenergic agonist
- salbutamol & ritodrine
-given IV infusion until
contraction stop/ maternal
heart rate > 140beat/min

B. Apomorphine sublingual
Centrally acting drug
Dopamine agonist mainly D2
Improve erectile function by enhancing the
natural central erectile signals that normally
occurs during sexual stimulation
Lower efficacy and satifiscation than sildenafil
st
1 line treatment in patients using nitrates
nd




4. NSAIDs ; Indomethacin
- inhibit production of
prostaglandins
- given as single rectal dose
then orally every 6hrs

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2 line therapy : injectible VD
Patients which not responding to oral drugs
Self injected directly into corpora cavernosa
Site ; dorsalateral aspects of proximal third of
the penis
Injected drugs :
A) papaverine
- non specific PDE inhibitor
- can be combined with phentolamine (alpha
adrenoreceptor antagonist)
B) alprostadil
-PGE1 analog
- mini suppository from which it diffuse into
corpora cavernosa
Adverse effect
Fibrosis at injection sites  should stop
injecting till fibrosis resolve  avoid penile
curvature
Priapism : erection last more than 1 hr
(urologic emergency)
Treatment :
Analgesic for pain
Sedative for anxiety
Aspirate blood from cavernosa
Intracavernosa administration of VC as
phenylephrine  Dose reduced for the next
injection