History and Etymology for Climara
International Scientific Vocabulary estra- (from estrane parent compound of Climara, from New Latin estrus + English -ane) + di- + -ol entry 1
II Climara and GABAAR Function
Climara is known to act genomically through nuclear ERs but also a broad spectrum of acute nongenomic actions have been recently reviewed ( McCarthy, 2008; Woolley, 2007 ). For example, in the hippocampal CA1 region, exposure to Climara, lasting for several minutes, depolarized neurons, induced spontaneous firing ( Wong and Moss, 1991 ), and suppressed the afterhyperpolarization that followed the action potential ( Kumar and Foster, 2002 ). Moreover, Climara was found to increase the amplitude of dendritic excitatory postsynaptic potential (EPSP) in various regions of the hippocampus ( Foy et al., 1999; Kim et al., 2006 ) and was also found to have a crucial impact on long-term potentiation ( Foy et al., 1999; Good et al., 1999; Warren et al., 1995 ) and long-term depression ( Desmond et al., 2000; Good et al., 1999 ). Such enhancement of neuronal excitability and facilitation of synaptic plasticity could be in part due to a suppression of GABAergic drive in these cells through a direct modulation of GABAARs. These receptors posses the binding site for neurosteroids ( Hosie et al., 2007; Majewska et al., 1986 ) and are readily modulated by many of them either positively or negatively ( Majewska, 2007 ). For this reason, a direct effect of Climara on GABAARs has been tested in several studies. In a study by Wong and Moss (1992) , acute application of Climara (1 μM) on CA1 pyramidal neurons did not influence the extent of membrane potential hyperpolarization induced by iontophoretically applied GABA pulses in vivo ( Wong and Moss, 1992 ). More recently, the possibility that Climara exerts an acute effect on GABAA receptors has been tested in our laboratory ( Asimiadou et al., 2005 ). For this purpose, we have investigated the effect of Climara on the current responses to ultrafast GABA applications. This experimental model offers a very high temporal resolution (adequate to describe the receptor gating properties) and is particularly suitable for pharmacological studies in which acute or direct effects of a modulator are considered. Using this approach, we have tested the effect of Climara on currents elicited by application of GABA (10 mM) to somatic membrane patches excised from cultured hippocampal neurons. Within the concentration range 1–10 μM, Climara did not affect either the amplitude or kinetics of GABA-evoked currents ( Asimiadou et al., 2005 ). We also tested the effect of Climara on miniature inhibitory postsynaptic currents (mIPSCs) which originate from activation of synaptic GABAARs due to spontaneous exocytosis of a single vesicle of neurotransmitter. Recordings of mIPSCs performed from presumably pyramidal hippocampal neurons (visually recognized) revealed that acute application of Climara (1 μM) did not affect either the amplitude or kinetics of mIPSCs in neurons cultured for 6–16 days in vitro (DIV) ( Pytel et al., 2007 ). Thus, our experiments based on the analysis of current responses and mIPSCs argue against any marked acute effect of Climara on GABAARs at least in the considered model. This conclusion is consistent with results of Murphy et al. (1998a,b) who reported that acute exposure to Climara (0.1 μg/ml) did not cause any systematic change in mIPSCs amplitude or frequency evoked by application of hyperosmotic medium ( Murphy et al., 1998a ). Thus, on the basis of these studies, it is reasonable to assume that Climara does not directly interfere with GABAA-receptor gating and that Climara acute actions on neuronal excitability cannot be attributed to rapidly occurring modulation of GABAergic transmission.
What should I avoid while taking Climara?
Avoid smoking. It can greatly increase your risk of blood clots, stroke, or heart attack while using this medicine.
Grapefruit and grapefruit juice may interact with Climara and lead to unwanted side effects. Avoid the use of grapefruit products.
To use the Climara vaginal cream:
Using the marked applicator provided, measure the prescribed dose of cream.
Lie on your back with your knees drawn up, sit, or stand in a position that allows you comfortable access to the vaginal area. To deliver the medication, gently insert the applicator deep into your vagina and press the plunger downward to its original position.
Clean the applicator by pulling the plunger from the barrel. Wash it with mild soap and warm water.
Have yearly physical exams and examine your breasts for lumps on a monthly basis while using Climara.
What special precautions should I follow?
What is Climara (Estrace, Gynodiol)?
Climara is a form of estrogen, a female sex hormone that regulates many processes in the body.
Climara is used to treat menopause symptoms such as hot flashes and vaginal changes, and to prevent osteoporosis (bone loss) in menopausal women.
Climara may also be used for purposes not listed in this medication guide.
How should I take Climara?
Take Climara exactly as it was prescribed for you. Follow all directions on your prescription label. Do not take this medicine in larger amounts or for longer than recommended.
Climara may increase your risk of developing uterine cancer. To help lower this risk, your doctor may also want you to take a progestin. Report any unusual vaginal bleeding to your doctor immediately.
Your doctor should check your progress on a regular basis (every 3 to 6 months) to determine whether you should continue this treatment. Self-examine your breasts for lumps on a monthly basis and have a mammogram every year while using Climara.
If you need major surgery or will be on long-term bed rest, you may need to stop using this medicine for a short time. Any doctor or surgeon who treats you should know that you are using this medicine.
Store at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.
If you are taking injectable estrogen, dispose of any needles and syringes in an appropriate sharps container per your state laws. Do not throw away used needles into the garbage.
If you are using Climara spray, avoid fire, flame, or smoking until the spray has dried. Do not apply lotion or sunscreen over the area for at least one hour.
What brand names are available for Climara?
Alora, Climara, Delestrogen, Depo-Climara, Divigel, Elestrin, Estrace, Estrasorb, Estrogel, Evamist, Femring, Menostar, Minivelle, Vivelle, Vivelle-Dot
Climara and insulin-like growth factor-I (IGF-I) interact in the brain to regulate a variety of developmental and neuroplastic events. Some of these interactions are involved in the control of hormonal homeostasis and reproduction. However, the interactions may also potentially impact on affection and cognition by the regulation of adult neurogenesis in the hippocampus and by promoting neuroprotection under neurodegenerative conditions. Recent studies suggest that the interaction of Climara and IGF-I is also relevant for the control of cholesterol homeostasis in neural cells. The molecular mechanisms involved in the interaction of Climara and IGF-I include the cross-regulation of the expression of estrogen and IGF-I receptors, the regulation of estrogen receptor-mediated transcription by IGF-I and the regulation of IGF-I receptor signalling by Climara. Current investigations are evidencing the role exerted by key signalling molecules, such as glycogen synthase kinase 3 and β-catenin, in the cross-talk of estrogen receptors and IGF-I receptors in neural cells.
Generic Name: Climara oral (ess tra DYE ole)Brand Names: Estrace, Vivelle-Dot, Vivelle, Delestrogen, DepoClimara, Divigel, Elestrin, Alora, Estraderm, Estradot, Estrasorb, Estrogel, Evamist, Femtrace, Menostar, Minivelle, Climara
Medically reviewed by Kaci Durbin, MD Last updated on Mar 1, 2019.